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All Pharm 1 liners

LECOM 2012 All Pharm 1 liners

Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs) Half-life (T1/2)
Relates the amount of drug in the body to the plasma concentration Volume of distribution (VD)
Plasma concentration of a drug at a given time Cp
The ratio of the rate of elimination of a drug to its plasma concentration Clearance (CL)
The elimination of drug that occurs before it reaches the systemic circulation First pass effect
The fraction of administered dose of a drug that reaches systemic circulation Bioavailability (F)
When the rate of drug input equals the rate of drug elimination Steady state
Metabolism This step of metabolism makes drug more hydrophilic and hence augments elimination Phase I
Different steps of Phase I Oxidation, reduction, hydrolysis
Inducers of Cytochrome P450 (CYP450) Barbiturates, phenytoin, carbamazepine, and rifampin
Inhibitors of CYP450 Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Products of Phase II conjugation Glucuronate, acetic acid, and glutathione sulfate
Constant percentage of substrate metabolized per unit time First order kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration Zero order kinetics
Target plasma concentration times (volume of distribution divided by bioavailability) Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided by bioavailability) Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor Affinity
Selectivity of a drug for its receptor Specificity
Amount of drug necessary to elicit a biologic effect Potency
Ability of drug to produce a biologic effect Efficacy
Ability of a drug to produce 100% of the maximum response regardless of the potency Full agonist
Ability to produce less than 100% of the response Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system Competitive antagonist
Ability to bind to either the same or different site as the drug Noncompetitive antagonist
Mechanism of action (MOA) utilizes intracellular receptors Thyroid and steroid hormones
MOA utilizes transmembrane receptors Insulin
MOA utilizes ligand gated ion channels Benzodiazepines and calcium channel blockers
Median effective dose required for an effect in 50% of the population ED50
Median toxic dose required for a toxic effect in 50% of the population TD50
Dose which is lethal to 50% of the population LD50
Window between therapeutic effect and toxic effect Therapeutic index
Drug with a high margin of safety High therapeutic index
Drug with a narrow margin of safety Low therapeutic index
Antidotes and agents used in drug overdose Antidote used for lead poisoning Dimercaprol, EDTA
Antidote used for cyanide poisoning Nitrites
Antidote used for anticholinergic poisoning Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity Deferoxamine
Antidote used for acetaminophen (APAP) toxicity N-acetylcysteine (Mucomyst)
Antidote for arsenic, mercury, lead, and gold poisoning Dimercaprol
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic Penicillamine
Antidote used for heparin toxicity Protamine
Antidote used for warfarin toxicity Vitamin and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase Aminocaproic acid
Antidote used for methanol and ethylene glycol Ethanol
Antidote used for opioid toxicity Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity Flumazenil
Antidote used for tricyclic antidepressants (TCA) Sodium bicarbonate
Antidote used for carbon monoxide poisoning 100% O2 and hyperbaric O2
Antidote used for digitalis toxicity Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol) Esmolol
Antidote for methotrexate toxicity Leucovorin
Antidote for beta-blockers and hypoglycemia Glucagon
Antidote useful for some drug induced Torsade de pointes Magnesium sulfate
Antidote for hyperkalemia sodium polystyrene sulfonate (Kayexalate)
Antidote for salicylate intoxication Alkalinize urine, dialysis
Cancer Chemotherapy Constant proportion of cell population killed rather than a constant number Log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously Pulse therapy
Toxic effect of anticancer drug can be lessened by rescue agents Rescue therapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates Allopurinol
Pyrimidine analog that causes "Thiamine-less death" given with leucovorin rescue 5-flouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms Prednisone
Side effect of Mitomycin SEVERE myelosuppression
MOA of cisplatin Alkylating agent
Common toxicities of cisplatin Nephro and ototoxicity
Analog of hypoxanthine, needs HGPRTase for activation 6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6-MP Allopurinol
May protect against doxorubicin toxic by scavenging free radicals Dexrazoxane
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis Bleomycin
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm Testicular cancer
MOPP regimen used in Hodgkin's disease (HD) Mechlorethamine+ oncovorin (vincristine)+ procarbazine, and prednisone
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
Regimen used for non-Hodgkin's lymphoma COP (cyclophosphamide, oncovin(vincristine), and prednisone)
Regimen used for breast cancer CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation Mechlorethamine
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis Cyclophosphamide
Prevention of cyclophosphamide induced hemorrhagic cystitis Hydration and mercaptoethanesulfonate (MESNA)
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation Vincristine
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase Paclitaxel (taxol)
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides Cisplatin
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression Carboplatin
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine) L-asparaginase
Used for hairy cell leukemia; it stimulates NK cells Interferon alpha
Anti-androgen used for prostate cancer Flutamide (Eulexin)
Anti-estrogen used for estrogen receptor + breast cancer Tamoxifen
Newer estrogen receptor antagonist used in advanced breast cancer Toremifene (Fareston)
Some cell cycle specific anti-cancer drugs Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle non-specific drugs Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist Odansetron, granisetron
Nitrosoureas with high lipophilicity, used for brain tumors Carmustine (BCNU) and lomustine (CCNU)
Produces disulfiram-like reaction with ethanol Procarbazine
Endocrine drugs: hypothalamic and pituitary hormones Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors Octreotide
Somatotropin (GH) analog used in GH deficiency (dwarfism) Somatrem
GHRH analog used as diagnostic agent Sermorelin
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively Leuprolide
GnRH antagonist with more immediate effects, used for infertility Ganirelix
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia Bromocriptine
Hormone inhibiting prolactin release Dopamine
ACTH analog used for diagnosis of patients with corticosteroid abnormality Cosyntropin
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis Desmopressin (DDAVP)
Thyroid and anti-thyroid drugs Most widely used thyroid drugs such as Synthroid and Levoxyl contain L-thyroxine (T4)
T3 compound less widely used Cytomel
Anti-thyroid drugs Thioamides, iodides, radioactive iodine, and ipodate
Thioamide agents used in hyperthyroidism Methimazole and propylthiouracil (PTU)
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy PTU
PTU (propylthiouracil) MOA Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism Iodide salts
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy Radioactive iodine
Radio contrast media that inhibits the conversion of T4 to T3 Ipodate
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3 Beta-blockers such as propranolol
Adrenocorticosteroid and adrenocortical antagonists 3 zones of adrenal cortex and their products Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
Pneumonic for 3 zones of adrenal cortex GFR
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation) Glucocorticoids
Short acting GC's Cortisone and hydrocortisone (equivalent to cortisol)
Intermediate acting GC's Prednisone, methylprednisolone, prednisolone, and triamcinolone
Long acting GC's Betamethasone, dexamethasone, and paramethasone
Mineralocorticoids Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroids Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis
Period of time of therapy after which GC therapy will need to be tapered 5-7 days
Inhibitors of corticosteroids biosynthesis Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test Metyrapone
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis Aminoglutethimide
Antifungal agent used for inhibition of all gonadal and adrenal steroids Ketoconazole
Antiprogestin used as potent antagonist of GC receptor Mifepristone
Diuretic used to antagonize aldosterone receptors Spironolactone
Common SE of spironolactone Gynecomastia and hyperkalemia
Gonadal hormones and inhibitors Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss Estrogen
Antiestrogen drugs used for fertility and breast cancer respectively Clomiphene and tamoxifen
Common SE of tamoxifen and raloxifene Hot flashes
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study) Raloxifene
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy Diethylstilbestrol (DES)
Estrogen mostly used in oral contraceptives (OC) Ethinyl estradiol and mestranol
Anti-progesterone used as abortifacient Mifepristone (RU-486)
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep) Combination oral contraceptives (OC)
Oral contraceptive available in a transdermal patch Ortho-Evra
Converted to more active form DHT by 5 alpha-reductase Testosterone
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness Finasteride (Proscar and Propecia respectively)
Anabolic steroid that has potential for abuse Nandrolone and stanozolol
Anti-androgen used for hirsutism in females Cyproterone acetate
Drug is used with testosterone for male fertility Leuprolide
Pancreatic hormones, antidiabetics, and hyperglycemics Alpha cells in the pancreas Produce glucagon
Beta cells in the pancreas Produce insulin
Beta cells are found Islets of Langerhans
Delta cells in the pancreas Produce Somatostatin
Product of proinsulin cleavage used to assess insulin abuse C-peptide
Exogenous insulin Little C-peptide
Endogenous insulin Normal C-peptide
Very rapid acting insulin, having fastest onset and shortest duration of action Lispro (Humalog)
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia Regular (Humulin R)
Long acting insulin Ultralente (humulin U)
Ultra long acting insulin, has over a day duration of action Glargine (Lantus)
Major SE of insulin Hypoglycemia
Important in synthesis of glucose to glycogen in the liver GLUT 2
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation GLUT 4
Examples of alpha-glucosidase inhibitors (AGI) Acarbose, miglitol
MOA of AGI's Act on intestine, delay absorption of glucose
SE of AGI's Flatulence (do not use beano to tx), diarrhea, abdominal cramps
Alpha-glucosidase inhibitor associated with elevation of LFT's Acarbose
Amino acid derivative Nateglinide
MOA of nateglinide Insulin secretagogue
Biguanide Metformin
Drugs available in combination with metformin Glyburide, glipizide, and rosiglitazone
MOA of metformin Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
Most important potential SE of metformin Lactic acidosis
Meglitinide Repaglinide
MOA of repaglinide Insulin release from pancreas; faster and shorter acting than sulfonylurea
First generation sulfonylurea Chlorpropamide, tolbutamide, tolazamide, etc.
Second generation sulfonylurea Glyburide, glipizide, glimepiride, etc.
MOA of both generations Insulin release from pancreas by modifying K+ channels
Common SE of sulfonylureas, repaglinide, and nateglinide Hypoglycemia
Sulfonylurea NOT recommended for elderly because of very long half life Chlorpropamide
Thiazolidinediones Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
Reason troglitazone was withdrawn from market Hepatic toxicity
MOA of thiazolindinediones Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
SE of Thiazolindinediones Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation Glucagon
Drugs used in bone homeostasis Available bisphosphonates Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates Inhibits osteoclast bone resorption
Only bisphosphonates available IV Etidronate
Uses of bisphosphonates Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
Major SE of bisphosphonates Chemical esophagitis
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia Etidronate
Used for prevention of postmenopausal osteoporosis in women Estrogen (HRT-Hormone replacement therapy)
Increase bone density, also being tested for breast CA tx. Raloxifene (SERM-selective estrogen receptor modulator)
Used intranasally and decreases bone resorption Calcitonin (salmon prep)
Used especially in postmenopausal women, dosage should be 1500 mg Calcium
Vitamin given with calcium to ensure proper absorption Vitamin D
Drugs with important actions on smooth muscle Disease caused by excess ergot alkaloids St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides Autocoids
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea Zollinger-Ellison Syndrome
Drug that causes contraction of the uterus Oxytocin
Distribution of histamine receptors H1, H2, and H3 Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
Prototype antagonist of H1 and H2 receptors Diphenhydramine
1st generation antihistamine that is highly sedating Diphendydramine
1st generation antihistamine that is least sedating Chlorpheniramine or cyclizine
2nd generation antihistamines Fexofenadine, loratadine, and cetirizine
Generation of antihistamine that has the most CNS effects First generation due to being more lipid-soluble
Major indication for H1 receptor antagonist Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and is not addictive hydroxyzine (Atarax)
H1 antagonist used in motion sickness Dimenhydrinate, meclizine, and other 1st generation
Most common side effect of 1st generation antihistamines Sedation
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme. Terfenadine and astemizole (have been removed from the market)
H2 blocker that causes the most interactions with other drugs Cimetidine
Clinical use for H2 blockers Acid reflux disease, duodenal ulcer and peptic ulcer disease
Receptors for serotonin (5HT-1) are located Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
" 5HT-1d agonist used for migraine headaches " Sumatriptan, naratriptan, and rizatriptan
Triptan available in parenteral and nasal formulation Sumatriptan
H1 blocker that is also a serotonin antagonist Cyproheptadine
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors)
Agents for reduction of postpartum bleeding Ergonovine and ergotamine
Agents used in treatment of carcinoid tumor Ketanserin cyproheptadine, and phenoxybenzamine
"5HT-3 antagonist used in chemotherapeutic induced emesis " "Ondansetron, granisetron, dolasetron and alosetron "
5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease Dolasetron
DOC of chemo induced nausea and vomiting Odansetron
Drug used in ergot alkaloids overdose, ischemia and gangrene Nitroprusside
Reason ergot alkaloids are contraindicated in pregnancy Uterine contractions
SE of ergot alkaloids Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug LSD
Dopamine agonist used in hyperprolactinemia Bromocriptine
Peptide causing increased capillary permeability and edema Bradykinin and histamine
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema Bradykinin
Drug causing depletion of substance P (vasodilator) Capsaicin
Prostaglandins that cause abortions Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
" Difference between COX 1 and COX 2 " "COX 1 is found throughout the body and COX 2 is only in inflammatory tissue"
Drug that selectively inhibits COX 2 Celecoxib, valdecoxib, and rofecoxib
Inhibitor of lipoxygenase Zileuton
Major SE of zileuton Liver toxicity
Inhibitor of leukotrienes (LTD4) receptors and used in asthma Zafirlukast and montelukast
Used in pediatrics to maintain patency of ductus arteriosis PGE1
Approved for use in severe pulmonary HTN PGI2 (epoprostenol)
Prostaglandin used in the treatment impotence Alprostadil
Irreversible, nonselective COX inhibitor Aspirin
Class of drugs that reversibly inhibit COX NSAIDS
Primary endogenous substrate for Nitric Oxidase Synthase Arginine
MOA and effect of nitric oxide Stimulates cGMP which leads to vascular smooth muscle relaxation
Long acting beta 2 agonist used in asthma Salmeterol
Muscarinic antagonist used in asthma Ipratropium
MOA action of cromolyn Mast cell stabilizer
Enzyme which theophylline inhibits Phosphodiesterase
Methylxanthine derivative used as a remedy for intermittent claudication Pentoxifylline
Antidote for severe CV toxicity of theophylline Beta blockers
" MOA of corticosteroids" inhibit phospholipase A2
SE of long term (>5 days) corticosteroid therapy and remedy Adrenal suppression and weaning slowly, respectively
Antimicrobials MOA of quinolones Inhibit DNA gyrase
MOA of penicillin Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
Drug used for MRSA Vancomycin
Vancomycin MOA Blocks peptidoglycan synthesis
Type of resistance found with vancomycin Point mutation
Meningitis prophylaxis in exposed patients Rifampin
Technique used to diagnose perianal itching, and the drug used to treat it "Scotch tape technique and mebendazole"
Two toxicities of aminoglycosides nephro and ototoxicity
DOC for Legionnaires' disease Erythromycin
MOA of sulfonamides Inhibit dihydropteroate synthase
Penicillins active against penicillinase secreting bacteria Methicillin, nafcillin, and dicloxacillin
Cheap wide spectrum antibiotic DOC of otitis media Amoxicillin
Class of antibiotics that have 10% cross sensitivity with penicillins Cephalosporins
PCN active against pseudomonas Carbenicillin, piperacillin and ticarcillin
Antibiotic causing red-man syndrome, and prevention "Vancomycin, infusion at a slow rate and antihistamines"
Drug causes teeth discoloration Tetracycline
MOA of tetracycline Decreases protein synthesis by inhibiting 30S ribosome
Drug that causes gray baby syndrome and aplastic anemia Chloramphenicol
Drug notorious for causing pseudomembranous colitis Clindamycin
DOC for tx of pseudomembranous colitis Metronidazole
Treatment of resistant pseudomembranous colitis ORAL vancomycin
Anemia caused by trimethoprim Megaloblastic anemia
Reason fluoroquinolones are contraindicated in children and pregnancy Cartilage damage
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas Metronidazole
Treatment for TB patients (think RIPE) Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
Metronidazole SE if given with alcohol Disulfiram-like reaction
Common side effect of Rifampin Red urine discoloration
MOA of nystatin Bind ergosterol in fungal cell membrane
Neurotoxicity with isoniazid (INH) prevented by Administration of Vit. B6 (pyridoxine)
Toxicity of amphotericin Nephrotoxicity
SE seen only in men with administration of ketoconazole Gynecomastia
Topical DOC in impetigo Topical mupirocin (Bactroban)
DOC for influenza A Amantadine
DOC for RSV Ribavirin
DOC for CMV retinitis Ganciclovir
SE for ganciclovir Neutro, leuko and thrombocytopenia
Anti-viral agents associated with Stephen Johnson syndrome Nevirapine, amprenavir HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism Protease inhibitors
Antivirals that are teratogens Delavirdine, efavirenz, and ribavirin
Antivirals associated with neutropenia Ganciclovir, zidovudine, saquinavir, and interferon
HIV med used to reduce transmission during birth AZT (zidovudine)
Drug used for African sleeping sickness Suramin
Drug used in Chagas disease Nifurtimox
Cephalosporins able to cross the BBB Cefixime (2nd) and 3rd generation
Drug used for N. gonorrhea in females Ceftriaxone
Cephalosporin causes kernicterus in neonates Ceftriaxone or cefuroxime
SE of INH Peripheral neuritis and hepatitis
Aminoglycoside that is least ototoxic Streptomycin
Drug used in exoerythrocytic cycle of malaria Primaquine
Oral antibiotic of choice for moderate inflammatory acne Minocycline
Drug of choice for leprosy Dapsone
DOC for herpes and its MOA Acyclovir and inhibits thymidine kinase Acyclovir and inhibits thymidine kinase
Anti-microbials that cause hemolysis in G6PD-deficient patients Sulfonamides
MOA of erythromycin Inhibition of protein synthesis at the 50s subunit of ribosome
Anti-biotic frequently used for chronic UTI prophylaxis sulfamethoxazole/ trimethoprim
Lactam that can be used in PCN allergic patients Aztreonam
SE of imipenem Seizures
Anti-viral with a dose limiting toxicity of pancreatitis Didanosine
Sedative Hypnotics Common side effect of hypnotic agents Sedation
Occurs when sedative hypnotics are used chronically or at high doses Tolerance
The most common type of drug interaction of sedative hypnotics with other depressant medications Additive CNS depression
Benzodiazepines Major effect of benzodiazepines on sleep at high doses REM is decreased
Neurologic SE of benzodiazepines Anterograde amnesia
Reason benzos are used cautiously in pregnancy Ability to cross the placenta
Main route of metabolism for benzodiazepines Hepatic
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired) Lorazepam, oxazepam, and temazepam
"MOA for benzodiazepines " increase the FREQUENCY of GABA-mediated chloride ion channel opening
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects) Flumazenil
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin Diazepam
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia Clonazepam
Benzodiazepines that are the most effective in the treatment of panic disorder Alprazolam and Clonazepam
"Benzodiazepine that is used for anesthesia " Midazolam
DOC for status epilepticus Diazepam
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs Chlordiazepoxide and Diazepam
Agents having active metabolites, long half lives, and a high incidence of adverse effects Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
Barbiturates Barbiturates may precipitate this hematologic condition Acute intermittent porphyria
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property Liver enzyme INDUCTION
Barbiturates MOA Increase the DURATION of GABA-mediated chloride ion channels
Barbiturate used for the induction of anesthesia Thiopental
Alcohols Important drug interaction with chloral hydrate May displace coumadin from plasma proteins
Others Site of action for zaleplon and zolpidem Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
Good hypnotic activity with less CNS SE than most benzodiazepines Zolpidem, zaleplon
Agent that is a partial agonist for the 5-HT1A receptor Buspirone
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety Buspirone
Alcohols Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS) Ethanol
Agent with zero-order kinetics Ethanol
Rate limiting step of alcohol metabolism Aldehyde dehydrogenase
System that increases in activity with chronic exposure and may contribute to tolerance MEOS
Agent that metabolize acetaldehyde to acetate Aldehyde dehydrogenase
Agents that inhibit alcohol dehydrogenase Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension Disulfiram
The most common neurologic abnormality in chronic alcoholics Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
Agent that is teratogen and causes a fetal syndrome Alcohol
Agent that is the antidote for methanol overdose Alcohol
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure Fomepizole
Anti seizure Drugs Most frequent route of metabolism Hepatic enzymes
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine Sodium blockade
MOA for benzodiazepines and barbiturates GABA-related targets
MOA for Ethosuximide Calcium channels
MOA for Valproic acid at high doses Affect calcium, potassium, and sodium channels
Drugs of choice for generalized tonic-clonic and partial seizures Valproic acid and Phenytoin
DOC for febrile seizures Phenobarbital
Drugs of choice for absence seizures Ethosuximide and valproic acid
Drug of choice for myoclonic seizures Valproic acid
Drugs of choice for status epilepticus IV diazepam or phenytoin (for prolonged therapy not acute)
Drugs that can be used for infantile spasms Corticosteroids
Anti-seizure drugs used also for bipolar affective disorder (BAD) Valproic acid, carbamazepine, phenytoin and gabapentin
Anti-seizure drugs used also for Trigeminal neuralgia Carbamazepine
Anti-seizure drugs used also for pain of neuropathic orgin Gabapentin
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism Phenytoin
SE of phenytoin Gingival hyperplasia, nystagmus, diplopia and ataxia
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida Carbamazepine
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress Valproic acid
Laboratory value required to be monitored for patients on valproic acid Serum ammonia and LFT's
SE for Lamotrigine Stevens-Johnson syndrome
SE for Felbamate Aplastic anemia and acute hepatic failure
Anti-seizure medication also used in the prevention of migraines Valproic acid
Carbamazepine may cause Agranulocytosis
Anti-seizure drugs used as alternative drugs for mood stabilization Carbamazepine, gabapentin, lamotrigine, and valproic acid
General Anesthetics MOA of general anesthetics Unclear, thought to increase the threshold for firing of CNS neurons
Inhaled anesthetic with a low blood/gas partition coefficient Nitrous oxide
Inversely related to potency of anesthetics Minimum alveolar anesthetic concentration (MAC)
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents Halothane and methoxyflurane
Most inhaled anesthetics SE Decrease arterial blood pressure
Inhaled anesthetics are myocardial depressants Enflurane and halothane
Inhaled anesthetic causes peripheral vasodilation Isoflurane
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis Halothane
Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration Nitrous oxide
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency Methoxyflurane
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia Nitrous oxide
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm Desflurane
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics Dantrolene
IV barbiturate used as a pre-op anesthetic Thiopental
Benzodiazepine used adjunctively in anesthesia Midazolam
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose Flumazenil
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery Ketamine
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia Fentanyl
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide Neuroleptanesthesia
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension Propofol
Local Anesthetics MOA of local anesthetics (LA's) Block voltage-dependent sodium channels
This may enhance activity of local anesthetics Hyperkalemia
This may antagonize activity of local anesthetics Hypercalcemia
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity Vasodilation
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery Cocaine
Longer acting local anesthetics which are less dependent on vasoconstrictors Tetracaine and bupivacaine
These LA's have surface activity Cocaine and benzocaine
Most important toxic effects of most local anesthetics CNS toxicity
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction Cocaine
LA causing methemoglobinemia Prilocaine
Skeletal Muscle Relaxants Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation Neuromuscular blocking drugs
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB) Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine) Nondepolarizing type antagonists
Agent with long duration of action and is sost likely to cause histamine release Tubocurarine
Non-depolarizing antagonist has short duration Mivacurium
Agent can blocking muscarinic receptors Pancuronium
Agent undergoing Hofmann elimination (breaking down spontaneously) Atracurium
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, xcuses muscle pain postoperatively and myoglobinuria may occur Succinylcholine
During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine Cholinesterase inhibitors
Spasmolytic drugs Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease Spasmolytic drugs
Facilitates GABA presynaptic inhibition Diazepam
GABA agonist in the spinal cord Baclofen
Similar to clonidine and may cause hypotension Tizanidine
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle Dantrolene
Agent used for acute muscle spasm Cyclobenzaprine
Drugs Used in Parkinsonism & Other Movement Disorders Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible Drug induced Parkinsonism
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB L-dopa
This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias) Carbidopa
Clinical response that may fluctuate in tx of Parkinson's dx "On-off-phenomenon"
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma Levodopa
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia Bromocriptine
Non ergot agents used as first-line therapy in the initial management of Parkinson's Pramipexole and ropinirole
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis Amantadine
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's Selegiline
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's) Entacapone and Tolcapone
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects Benztropine
Agent effective in physiologic and essential tremor Propranolol
Agents used in Huntington's Disease Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
Agents used in Tourette's dx Haloperidol or pimozide
Chelating agent used in Wilson's disease Penicillamine
Antipsychotics Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor Older antipsychotic agents, D2 receptors
Side effects occuring in antipsychotics that block dopamine Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
Antipsychotics that reduce positive symptoms only Older antipsychotics
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation Olanzapine, aripiprazole, and sertindole
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia Risperidone
Atypical antipsychotic causing high prolactin levels Risperidone
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes Olanzapine
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker Haloperidol
Drug used in neuroleptic malignant syndrome Dantrolene
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment) Muscarinic blockers Antipsychotic having the strongest autonomic effects Thioridazine
Antipsychotic having the weakest autonomic effects Haloperidol
Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval Sertindole
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias Thioridazine
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis Clozapine
Anti-psychotic not shown to cause tardive dyskinesia Clozapine
Anti-psychotics available in depot preparation Fluphenazine and haloperidol
Reduced seizure threshold Low-potency typical antipsychotics and clozapine
Orthostatic hypotension and QT prolongation Low potency and risperidone
Increased risk of developing cataracts Quetiapine
Lithium Major route of elimination for Lithium Kidneys
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop Lithium toxicity
Drug increases the renal clearance hence decreases levels of lithium Theophylline
Lithium is associated with this congenital defect Cardiac anomalies and is contraindicated in pregnancy or lactation
DOC for bipolar affective disorder Lithium
SE of lithium Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
Antidepressants Example of three antidepressants that are indicated for obsessive compulsive disorder Clomipramine, fluoxetine and fluvoxamine
Neurotransmitters affected by the action of antidepressants Norepinephrine and serotonin
Usual time needed for full effect of antidepressant therapy 2 to 3 weeks
Population group especially sensitive to side effects of antidepressants Elderly patients
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion Side-effect profile and prior pt response
Well-tolerated and are first-line antidepressants SSRI's, bupropion, and venlafaxine
Monoamine oxidase inhibitors (MAOI) Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression Monamine oxidase inhibitors
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats) Hypertensive crisis
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition Serotonin syndrome
Tricyclic antidepressants (TCA) Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly Tricyclic antidepressants (TCA)
Three C's associated with TCA toxicity Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
Agents having higher sedation and antimuscarinic effects than other TCA's Tertiary amines
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects Amitriptyline
TCA used in chronic pain, enuresis, and ADD Imipramine
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep Doxepin
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms Clomipramine
Secondary amines that have less sedation and more excitation effect Nortriptyline, Desipramine
Heterocyclics Antidepressant associated with neuroleptic malignant syndrome Amoxapine
Antidepressant associated with seizures and cardiotoxicity Maprotiline
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure Venlafaxine
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake Venlafaxine
Antidepressant also used for sleep that causes priapism Trazodone
Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure Nefazodone
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures Bupropion
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating Mirtazapine
SE of mirtazapine Liver toxicity, increased serum cholesterol
Selective serotonin reuptake inhibitors (SSRI) Except for these agents all SSRI have significant inhibition of CytP450 enzymes Citalopram and its metabolite escitalopram
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx Fluoxetine
SSRI indicated for premenstrual dysphoric disorder Fluoxetine (Sarafem)
Some of SSRIs' therapeutic effects beside depression Panic attacks, social phobias, bulimia nervosa, and PMDD premenstrual dysphoric disorder), OCD
SSRI's less likely to cause a withdrawal syndrome Fluoxetine
Opioid Analgesics & Antagonists Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons Ascending pathways
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release Presynaptic mu, delta, and kappa receptors
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization Postsynaptic Mu receptors
Tolerance to all effects of opioid agonists can develop except Miosis and constipation
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction Meperidine
SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone Opioid Analgesics
Strong opioid agonists Morphine, methadone, meperidine, and fentanyl
Opioids used in anesthesia Morphine and fentanyl
Opioid used in the management of withdrawal states Methadone
Opioid available trans-dermally Fentanyl
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema Morphine
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome Meperidine
Moderate opioid agonists Codeine, hydrocodone, and oxycodone
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures Propoxyphene
Partial agonist or mixed antagonists Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal Buprenorphine
Opioid antagonist that is given IV and had short DOA Naloxone
Opioid antagonist that is given orally in alcohol dependency programs Naltrexone
These agents are used as antitussive Dextromethorphan, Codeine
These agents are used as antidiarrheal Diphenoxylate, Loperamide
Drugs of Abuse Inhalant anesthetics NO, chloroform, and diethyl ether
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation Fluorocarbons and Industrial solvents
Cause dizziness, tachycardia, hypotension, and flushing Organic nitrites
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression Steroids
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
Opioid Analgesics Most commonly abused in health care professionals Heroin, morphine, oxycodone, meperidine and fentanyl
This route is associated with rapid tolerance and psychologic dependence IV administration
Leads to respiratory depression progressing to coma and death Overdose of opioids
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome Abstinence syndrome
Treatment for opioid addiction Methadone, followed by slow dose reduction
This agent may cause more severe, rapid and intense symptoms to a recovering addict Naloxone
Sedative-Hypnotics Sedative-Hypnotics action Reduce inhibition, suppress anxiety, and produce relaxation
Additive effects when Sedative-Hypnotics used in combination with these agents CNS depressants
Common mechanism by which overdose result in death Depression of medullary and cardiovascular centers
"Date rape drug" Flunitrazepam (rohypnol)
The most important sign of withdrawal syndrome Excessive CNS stimulation (seizures)
Treatment of withdrawal syndrome involves Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
These agents are CNS depressants Ethanol, Barbiturates, and Benzodiazepines
Stimulants Withdrawal from this drug causes lethargy, irritability, and headache Caffeine
W/D from this drug causes anxiety and mental discomfort Nicotine
Treatments available for nicotine addiction Patches, gum, nasal spray, psychotherapy, and bupropion
Chronic high dose abuse of nicotine leads to Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
Tolerance is marked and abstinence syndrome occurs Amphetamines
Amphetamine agents Dextroamphetamines and methamphetamine
These agents are congeners of Amphetamine DOM, STP, MDA, and MDMA "ecstasy"
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke) Cocaine "super-speed"
Hallucinogens Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic PCP
Removal of PCP may be aided Urinary acidification and activated charcoal or continual nasogastric suction
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur Marijuana
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention Bethanechol
Only direct acting agent that is very lipid soluble and used in glaucoma Pilocarpine
This agent used to treat dry mouth in Sjögren's syndrome Cevimeline
Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis Edrophonium
Carbamate with intermediate action postoperative and neurogenic ileus and urinary retention Neostigmine
Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions Physostigmine
Treatment of myasthenia gravis Pyridostigmine
Organophosphates Antiglaucoma organophosphate Echothiophate
Associated with an increased incidence of cataracts in patients treated for glaucoma Long acting cholinesterase inhibitors
Scabicide organophosphate Malathion
Organophosphate anthelmintic agent with long DOA Metrifonate
Toxicity of organophosphate: DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
The most important cause of acute deaths in cholinesterase inhibitor toxicity Respiratory failure
The most toxic organophosphate Parathion
Treatment of choice for organophosphate overdose Atropine
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure Pralidoxime
Cholinoreceptor Blockers & Cholinesterase Regenerators Prototypical drug is atropine Nonselective Muscarinic Antagonists
Treat manifestations of Parkinson's disease and EPS Benztropine, trihexyphenidyl
Treatment of motion sickness Scopolamine
Produce mydriasis and cycloplegia Atropine, homatropine tropicamide
Bronchodilation in asthma and COPD Ipratropium
Reduce transient hyper GI motility Dicyclomine, methscopolamine
Cystitis, postoperative bladder spasms, or incontinence Oxybutynin, dicyclomine
Toxicity of anticholinergics block SLUD (salivation, lacrimation, urination, defecation
Another pneumonic for anticholinergic toxicity "dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
Atropine fever is the most dangerous effect and can be lethal in this population group Infants
Contraindications to use of atropine Infants, closed angle glaucoma, prostatic hypertrophy
Nicotinic Antagonists Prototype ganglion blocker Hexamethonium
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate Severe hypertension
Reversal of blockade by neuromuscular blockers Cholinesterase inhibitors
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis Nondepolarizing Neuromuscular Blockers
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use Succinylcholine
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred) Cholinesterase Regenerators
Used to treat patients exposed to insecticides such as parathion Pralidoxime
Sympathomimetics Pneumonic for beta receptors You have 1 heart (Beta 1) and 2 lungs (Beta 2)
This is the drug of choice for anaphylactic shock Epinephrine
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction Amphetamines
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia Phenylephrine
Epinephrine and dipivefrin are used for Glaucoma
Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma Reduce aqueous synthesis
Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis Albuterol
Longer acting Beta 2 agonists is recommended for prophylaxis of asthma Salmeterol
These agents increase blood flow and may be beneficial in treatment of acute heart failure and some types of shock Beta1 agonists
These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion Alpha1 agonists
Shock due to septicemia or myocardial infarction is made worse by Increasing afterload and tissue perfusion declines
Often mixed with local anesthetic to Reduce the loss from area of injection
Chronic orthostatic hypotension can be treated with Midodrine
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus Terbutaline
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis Ephedrine
Alpha 1 agonist toxicity Hypertension
Beta 1 agonist toxicity Sinus tachycardia and serious arrhythmias
Beta 2 agonist toxicity Skeletal muscle tremor
The selective agents loose their selectivity at high doses
Adrenoceptor Blocker Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis Phenoxybenzamine
Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena Phentolamine
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension Prazosin, terazosin, doxazosin
Selective Alpha 2 blocker used for impotence (controversial effectiveness) Yohimbine
Beta-Blocking Drugs SelectiveB1 Receptor blockers that may be useful in treating patients with asthma Acebutolol, atenolol, esmolol, metoprolol
Combined alpha and beta blocking agents that may have application in treatment of CHF Labetalol and carvedilol
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma Pindolol and acebutolol
This beta blocker lacks local anesthetic activity (decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma Timolol
This parenteral beta blocker is a short acting Esmolol
This beta blocker is the longest acting Nadolol
These beta blockers are less lipid soluble Acebutolol and atenolol
This beta blocker is highly lipid soluble and may account for side effects such as nightmares Propranolol
Clinical uses of these agents include treatment of HTN, angina, arrhythmias, and chronic CHF Beta blockers
Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF, signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety) Beta blockers
Glaucoma (all agents topical except for diuretics) Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction Pilocarpine, carbachol, physostigmine
Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins Epinephrine, dipivefrin
Selective alpha agonists that decreases aqueous secretion Apraclonidine, brimonidine
These Beta blockers decrease aqueous secretion Timolol (nonselective), betaxolol (selective)
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis Acetazolamide
This agent cause increased aqueous outflow Prostaglandin PGF2a
Antihypertensive Agents Inhibit angiotensin-converting enzyme (ACE) Ace inhibitors
Captopril and enalapril (-OPRIL ending) are Ace inhibitors
SE of ACE inhibitors Dry cough, hyperkalemia
Ace inhibitors are contraindicated in pregnancy and with K+
Losartan and valsartan block Angiotensin receptor
Angiotensin receptor blockers do NOT cause Dry cough
Block L-type calcium channel Calcium channel blockers
CCB contraindicated in CHF Verapamil
CCB with predominate effect on arteriole dilation Nifedipine
SE of CCB Constipation, edema, and headache
Reduce heart rate, contractility, and O2 demand Beta-blockers
B-blockers that are more cardioselective Beta C2001-selective blockers
Cardioselective Beta 1-blockers Atenolol, acebutolol, and metoprolol
Beta-blockers should be used cautiously in Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
Non-selective Beta-blocker also used for migraine prophylaxis Propranolol
SE of beta blockers Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
Alpha 1selective blockers Prazosin, terazosin and doxazosin (-AZOSIN ending)
Non-selective Alpha1blockers use to treat pheochromocytoma Phenoxybenzamine
For rebound HTN from rapid clonidine withdrawal Phentolamine
A1a-selective blocker used for BPH Tamsulosin (Flomax)
SE of alpha blockers Orthostatic hypotension (especially with first dose) and reflex tachycardia
Presynaptic Alpha 2 agonist used in HTN Clonidine, and methyldopa
SE of methyldopa Positive Comb's test, depression
Methyldopa is contraindicated in Geriatrics due to its CNS (depression) effects
SE of clonidine Rebound HTN, sedation, dry mouth
Ganglionic blockers formerly used in HTN Trimethaphan, and hexamethonium
Direct vasodilator of arteriolar smooth muscle Hydralazine
SE of hydralazine Lupus-like syndrome
Arterial vasodilator that works by opening K+ channels Minoxidil
SE of minoxidil Hypertrichosis
IV Drug used Hypertensive Crisis Nitroprusside
Nitroprusside vasodilates Arteries and veins
Toxicity caused by nitroprusside and treatment Cyanide toxicity treated with sodium thiosulfate
Diuretics Carbonic anhydrase inhibitor Acetazolamide
Diuretic used for mountain sickness and glaucoma Acetazolamide
SE of acetazolamide Paresthesias, alkalization of the urine (which may ppt. Ca salts), hypokalemia, acidosis, and encephalopathy in patients with hepatic impairment
MOA of loop diuretics inhibits Na+/K+/2Cl- cotransport
Site of action of loop diuretics Thick ascending limb
SE of loop (furosemide) diuretics Hyperuricemia, hypokalemia and ototoxicity
Aminoglycosides used with loop diuretics potentiate adverse effect Ototoxicity
Loops lose and thiazide diuretics retain Calcium
MOA of thiazide diuretics Inhibit Na+/Cl- cotransport
Site of action of thiazide diuretics Work at early distal convoluted tubule
Class of drugs that may cause cross-sensitivity with thiazide diuretics Sulfonamides
SE of thiazide (HCTZ) diuretics Hyperuricemia, hypokalemia and hyperglycemia
Potassium sparing diuretics inhibit Na+/K+ exchange
Diuretic used to treat primary aldosteronism Spironolactone
SE of spironolactone Gynecomastia hyperkalemia, and impotence
Osmotic diuretic used for increased intracranial pressure Mannitol
Antidiuretic hormone (ADH) agonist and antagonist ADH agonist used for pituitary diabetes insipidus Desmopressin (DDAVP)
Used for SIADH Demeclocycline
SE of demeclocycline Bone marrow and teeth discoloration for children under 8 years of age
Antiarrhythmic agents MOA of class I A (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics Sodium channel blockers
SE of procainamide Lupus-like syndrome
Limiting side effect of Quinidine Prolongs QT interval
Other side effects of Quinidine Thrombocytopenic purpura, and CINCHONISM
Major drug interaction with Quinidine Increases concentration of Digoxin
DOC for management of acute Ventricular arrhythmias Lidocaine
DOC for digoxin induced arrhythmias Phenytoin
SE of phenytoin Gingival hyperplasia
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents Class IC (flecainide, propafenone, moricizine)
Class II antiarrhythmics are B-blockers
Antiarrhythmic that exhibits Class II and III properties Sotalol
Side effect of sotalol prolongs QT and PR interval
Used intravenously for acute arrhythmias during surgery Esmolol
Anti-arrhythmics that decrease mortality B-blockers
MOA of class III antiarrhythmics Potassium channel blockers
Class III antiarrhythmic that exhibits properties of all 4 classes Amiodarone
Specific pharmacokinetic characteristic of amiodarone Prolonged half-life, up to six weeks
Antiarrhythmic effective in most types of arrhythmia Amiodarone
SE of Amiodarone Dysfunction, photosensitivity, skin (blue smurf syndrome), Pulmonary fibrosis, thyroid and corneal deposits
MOA of class IV antiarrhythmics Calcium channel blockers
Life threatening cardiac event that prolong QT leads to Torsades de pointes
Agent to treat torsades de pointes Magnesium sulfate
Drug used supraventricular arrhythmias Digoxin
DOC for paroxysmal supraventricular tachycardia (PSVT) Adenosine
Adenosine's MOA Activates acetylcholine sensitive K+ channels in SA and AV node
Anti-arrhythmic with 15 second duration of action Adenosine
Vasodilators and treatment of angina MOA of sildenafil (Viagra) Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP
Drugs used in the management of angina Aspirin, Nitrates, CCB, and Beta blockers
Aspirin reduces mortality in unstable angina by Platelet aggregation inhibition
MOA of nitrates Relax vascular smooth muscle, at low doses dilate veins and at high doses dilate arterioles
Nitrate used for acute anginal attacks Nitroglycerin sublingual tablets
Nitrate used to prevent further attacks Oral and transdermal forms of nitroglycerin
Nitrate free intervals are needed due to Tolerance
SE of nitrates Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation
CCB are DOC for Prinzmetal's angina
Beta blockers are used for which type of anginal attack Classic
Drugs used to treat CHF MOA of Cardiac glycosides (eg. digoxin) Indirectly increase intracellular calcium and cardiac contractility by inhibit Na+/K+ ATPase
Digoxin is used in Atrial fibrillation and CHF
Digoxin toxicity can be precipitated by Hypokalemia
Antidote for digoxin toxicity Digibind
Phosphodiesterase inhibitors that increase mortality and have been found to have NO beneficial effects Amrinone and milrinone
SE of amrinone Thrombocytopenia
Beta 1 agonists used in acute CHF Dobutamine and dopamine
Diuretics work in CHF by Reducing preload
Beta blockers work in CHF by Reducing progression of heart failure (never use in acute heart failure)
Agent used in CHF that is a selective alpha and nonselective beta blocker Carvedilol
Agent used in acutely decompensated CHF resembling natriuretic peptide Nesiritide (Natrecor)
Drugs used in coagulation disorders Vitamin K dependent anticoagulant Warfarin (PT)
Warfarin is contraindicated in Pregnancy
Anticoagulant of choice in pregnancy Heparin
Heparin (PTT) increases activity of Antithrombin 3
Route of administration of warfarin Oral
Routes of administration of heparin IM (only LMW) and IV
SE of both warfarin and heparin Bleeding
SE of heparin Heparin induced thrombocytopenia (HIT)
Alternative anticoagulant used if HIT develops Lepirudin
Antidote to reverse actions of warfarin Vitamin K or fresh frozen plasma
Antidote to reverse actions of heparin Protamine sulfate
MOA of aspirin Irreversibly blocking cyclooxygenase
Agent used to treat MI and to reduce incidence of subsequent MI Aspirin
SE of Aspirin GI bleeding
Antiplatelet drug reserved for patients allergic to aspirin Ticlopidine
SE for ticlopidine Neutropenia and agranulocytosis
Effective in preventing TIA's Clopidogrel and ticlopidine
Prevents thrombosis in patients with artificial heart valve Dipyridamole
Block glycoprotein IIb/IIIa involved in platelet cross-linking Abciximab, tirofiban and eptifibatide
MOA of thrombolytics Degradation of fibrin clots and are administered
Thrombolytics are used for Pulmonary embolism and DVT
Thrombolytic that can cause allergic reaction Streptokinase
Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA Tissue plasmin activator
SE of tPA Cerebral hemorrhage
Antidote for thrombolytics Aminocaproic acid
Agents used in anemias and hematopoietic growth factors Agent to treat hypochromic microcytic anemias Ferrous sulfate
Chelating agent used in acute iron toxicity Deferoxamine
Agent for pernicious anemia Cyanocobalamin (Vit B12)
Agent used for neurological deficits in megaloblastic anemia Vitamin B12
Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy Folic acid
Agent used for anemias associated with renal failure Erythropoietin
Agent used neutropenia especially after chemotherapy G-CSF (filgrastim) and GM-CSF (sargramostim)
Treatment of patients with prior episodes of thrombocytopenia after a cycle of cancer chemotherapy Interleukin 11 (oprelvekin)
Antihyperlipidemics Decrease intestinal absorption of cholesterol Bile acid-binding resins
Cholestyramine and colestipol are Bile acid-binding resins
Major nutritional side effect of bile acid-binding resins Impair absorption of fat soluble vitamin absorption (A,D,E,K)
MOA of lovastatin (STATIN) inhibits HMG COA reductase
HMG CoA reductase inhibitors are contraindicated in Pregnancy
Drug or foods (grapefruit juice) that increase statin effect Inhibit Cytochrome P450 3A4
SE of HMG COA reductase inhibitors Rhabdomyolysis and Hepatotoxicity
Monitoring parameter to obtain before initiation of STATINS LFT's
Decreases liver triglycerol synthesis Niacin
SE of niacin Cutaneous flush
Cutaneous flush and be reduced by pretreatment with Aspirin
Fibrates (gemfibrozil) increase activity of Lipoprotein lipase
Most common SE of fibrates Nausea
Fibrates are contraindicated in Pregnancy
Concurrent use of fibrates and statins increases risk of Rhabdomyolysis
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins Ezetimibe (Zetia)
NSAIDS and DMARDS MOA of NSAIDS inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)
Difference between aspirin and other NSAIDS Aspirin irreversibly inhibits cyclooxygenase
Four main actions of NSAIDS Anti-inflammatory, analgesia, antipyretic and antiplatelet activity
Agent used for closure of patent ductus arteriosus Indomethacin
Aspirin is contraindicated in children with viral infection Potential for development of Reye's syndrome
SE of salicylates Tinnitus, GI bleeding
NSAID also available as an ophthalmic preparation Diclofenac
NSAID available orally, IM and ophthalmically Ketoralac
NSAID that is used for acute condition, such as pre-op anesthesia and has limited duration (<5 days) of use due to nephrotoxicity Ketoralac
Newer NSAIDs that selectively inhibit COX-2 Celecoxib and rofecoxib
COX 2 inhibitors may have reduced risk of Gastric ulcers and GI Bleeding
COX 2 inhibitors should be used cautiously in pts with Pre-existing cardiac or renal disease
Acetaminophen only has Antipyretic and analgesic activity
SE of acetaminophen Hepatotoxicity
Antidote for acetaminophen toxicity N-acetylcysteine
Drugs-Modifying Anti-Rheumatic Agents (DMARDS) DMARDs are slow acting drugs for Rheumatic disease
MOA of gold salts Alter activity of macrophages and suppress phagocytic activity of PMNs
SE of gold salts Dermatitis of the mouth aplastic anemia and agranulocytosis
Causes bone marrow suppression Methotrexate
SE of penicillamine Aplastic anemia and renal
Interferes with activity of T-lymphocytes Hydroxychloroquine
Anti-malarial drug used in rheumatoid arthritis (RA) Hydroxychloroquine
SE of hydroxychloroquine Retinal destruction and dermatitis
MOA of Leflunomide (newer agent) Inhibiting Dihydroorotate Dehydrogenase which leads to decreased pyrimidine synthesis
Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha) Infliximab and etanercept
Anti-rheumatic agent also used for ulcerative colitis Sulfasalazine
Drugs used in Gout NSAIDS used in gout Indomethacin and phenylbutazone
NSAID contraindicated in gout Aspirin
SE of phenylbutazone Aplastic anemia and agranulocytosis
MOA of Colchicine (used in acute gout) Selective inhibitor of microtubule assembly
SE of colchicine Kidney and liver toxicity
Agent used to treat chronic gout by increasing uric acid secretion Probenecid and sulfinpyrazone
Allopurinol treats chronic gout by inhibiting Xanthine oxidase
Created by: csheck