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Unstarred One Liners
Question | Answer |
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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 | |
Different steps of Phase I | Oxidation, reduction, hydrolysis |
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)) |
Pharmacodynamics | |
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 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 |
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 iron salt toxicity | Deferoxamine |
Antidote for severe lead poisoning | Dimercaprol + CaEDTA (edetate calcium disodium) |
Antidote for arsenic, mercury, and gold poisoning | Dimercaprol |
Antidote used in Wilson's disease (copper poisoning) | Penicillamine |
Antidote used for methanol and ethylene glycol | Ethanol |
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) |
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 |
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) |
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 |
Nitrosoureas with high lipophilicity, used for brain tumors | Carmustine (BCNU) and lomustine (CCNU) |
Alkylating agent that 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 |
Thyroid and anti-thyroid drugs | |
T3 compound less widely used | Cytomel |
Anti-thyroid drugs | Thioamides, iodides, radioactive iodine, and ipodate |
Thioamide agents used in hyperthyroidism | Methimazole and propylthiouracil (PTU) |
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 |
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 |
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 |
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 |
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 |
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 |
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) |
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 |
MOA of nateglinide | Stimulates rapid and transient release of of insulin through closure of the ATP-sensitive K+ channel |
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) |
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 |
1st generation antihistamine that is least sedating | Chlorpheniramine or cyclizine |
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) |
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 |
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) |
5ht-3 antagonist that has been MOST associated with QRS and QTc prolongation and should not be used in patients with heart disease | Dolasetron |
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 |
Peptide causing increased capillary permeability and edema | Bradykinin and histamine |
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 |
Major SE of zileuton | Liver toxicity |
Inhibitor of leukotrienes (LTD4) receptors and used in asthma | Zafirlukast and montelukast |
Approved for use in severe pulmonary HTN | PGI2 (epoprostenol) |
Irreversible, nonselective COX inhibitor | Aspirin |
Class of drugs that reversibly inhibit COX | NSAIDS |
Primary endogenous substrate for Nitric Oxidase Synthase | Arginine |
Long acting beta 2 agonist used in asthma | Salmeterol |
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 |
Antimicrobials | |
MOA of penicillin | Block cell wall synthesis by inhibiting peptidoglycan cross-linkage |
Type of resistance found with vancomycin | Point mutation |
Two toxicities of aminoglycosides | nephro and ototoxicity |
DOC for Legionnaires' disease | Erythromycin |
Penicillins active against penicillinase secreting bacteria | Methicillin, nafcillin, and dicloxacillin |
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 |
Treatment of resistant pseudomembranous colitis | ORAL vancomycin |
Reason fluoroquinolones are contraindicated in children and pregnancy | Cartilage damage |
Metronidazole SE if given with alcohol | Disulfiram-like reaction |
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 CMV retinitis | Ganciclovir |
SE for ganciclovir | Myelosuppression |
Anti-viral agents associated with Stephen Johnson syndrome | Nevirapine, amprenavir |
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 |
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 |
MOA of erythromycin | Inhibition of protein synthesis at the 50s subunit of ribosome |
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 | |
Neurologic SE of benzodiazepines | Anterograde amnesia |
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 |
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 with zero-order kinetics | Ethanol |
Rate limiting step of alcohol metabolism | Aldehyde dehydrogenase |
Agent that metabolize acetaldehyde to acetate | Aldehyde dehydrogenase |
Agents that inhibit aldehyde 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 |
Agent that is teratogen and causes a fetal syndrome | Alcohol |
Agent that competes for alcohol dehydrogenase in the case of methanol overdose | Ethanol |
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 |
DOC for febrile seizures | Phenobarbital |
Drugs of choice for status epilepticus | IV diazepam (or lorazapam) followed by phenytoin |
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 agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism | Phenytoin |
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 |
IV barbiturate used as a pre-op anesthetic | Thiopental |
Benzodiazepine used adjunctively in anesthesia | Midazolam |
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery | Ketamine |
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 |
Agent used for acute muscle spasm | Cyclobenzaprine |
Drugs Used in Parkinsonism & Other Movement Disorders | |
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 |
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 |
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 |
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment) | Muscarinic blockers |
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 |
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 | |
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 |
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 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 |
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 open K+ ion channels to cause membrane hyperpolarization | Postsynaptic Mu receptors |
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 |
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome | Meperidine |
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 |
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 |
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 |
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 |
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 |
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 |
Stimulants | |
Withdrawal from this drug causes lethargy, irritability, and headache | Caffeine |
W/D from this drug causes anxiety and mental discomfort | Nicotine |
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 |
Cholinoreceptor-Activating & Cholinesterase-Inhibiting Drugs | |
Direct-Acting Cholinomimetic Agonists | |
Muscarinic agonists or parasympathomimetic | |
Only direct acting agent that is very lipid soluble and used in glaucoma | Pilocarpine |
These agents are used to treat dry mouth in Sjögren's syndrome | Pilocarpine or 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 |
The most important cause of acute deaths in cholinesterase inhibitor toxicity | Respiratory failure |
The most toxic organophosphate | Parathion |
Treatment of muscarinic symptoms in 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 |
Reduce transient hyper GI motility | Dicyclomine, methscopolamine |
Cystitis, postoperative bladder spasms, or incontinence | Oxybutynin, dicyclomine |
Toxicity of anticholinergics | Anti-DUMBBELSS |
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 | |
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 |
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 |
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 2 blocker used for impotence (controversial effectiveness) | Yohimbine |
Beta-Blocking Drugs | |
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 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 |
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 | |
Block L-type calcium channel | Calcium channel blockers |
CCB with predominate effect on arteriole dilation | Nifedipine |
B-blockers that are more cardioselective | Beta C2001-selective blockers |
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 |
Non-selective Alpha1blockers use to treat pheochromocytoma | Phenoxybenzamine |
For rebound HTN from rapid clonidine withdrawal | Phentolamine |
Presynaptic Alpha 2 agonist used in HTN | Clonidine, and methyldopa |
SE of methyldopa | Positive Comb's test, depression |
SE of clonidine | Rebound HTN, sedation, dry mouth |
Ganglionic blockers formerly used in HTN | Trimethaphan, and hexamethonium |
Direct vasodilator of arteriolar smooth muscle | Hydralazine |
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 |
MOA of loop diuretics | inhibits Na+/K+/2Cl- cotransport |
Aminoglycosides used with loop diuretics potentiate adverse effect | Ototoxicity |
MOA of thiazide diuretics | Inhibit Na+/Cl- cotransport |
Class of drugs that may cause cross-sensitivity with thiazide diuretics | Sulfonamides |
Antidiuretic hormone (ADH) agonist and antagonist | |
Used for SIADH | Demeclocycline |
SE of demeclocycline | Bone marrow and teeth discoloration for children under 8 years of age |
Antiarrhythmic agents | |
Other side effects of Quinidine | Thrombocytopenic purpura, and CINCHONISM |
Major drug interaction with Quinidine | Increases concentration of Digoxin |
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 |
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 | |
Drugs used in the management of angina | Aspirin, Nitrates, CCB, and Beta blockers |
Aspirin reduces mortality in unstable angina by | Platelet aggregation inhibition |
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 | |
Warfarin is contraindicated in | Pregnancy |
Anticoagulant of choice in pregnancy | Heparin |
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 |
MOA of aspirin | Irreversibly blocking cyclooxygenase |
Agent used to treat MI and to reduce incidence of subsequent MI | Aspirin |
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 |
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 used for neurological deficits in megaloblastic anemia | Vitamin B12 |
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) |
inhibits HMG COA reductase | |
MOA of lovastatin (STATIN) | |
HMG CoA reductase inhibitors are contraindicated in | Pregnancy |
SE of HMG COA reductase inhibitors | Rhabdomyolysis and Hepatotoxicity |
Cutaneous flush and be reduced by pretreatment with | Aspirin |
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 |
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 |
SE of acetaminophen | Hepatotoxicity |
Drugs-Modifying Anti-Rheumatic Agents (DMARDS) | |
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 | |
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 |