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Combined Rx

Pharmacology One-lIners

QuestionAnswer
Antidote used for anticholinergic poisoning Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning Atropine, pralidoxime (2-PAM)
3 zones of adrenal cortex and their products Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid
Used for Addison's disease ,Congenital Adrenal Hyperplasia (CAH) , inflammation, allergies, and asthma (as a local inhalation) Cortisone and hydrocortisone (equivalent to cortisol)
Long acting glucocorticoids Betamethasone and dexamethasone
Mineralocorticoids Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroids Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
Period of time of therapy after which GC therapy will need to be tapered 5-7 days
Common SE of spironolactone Gynecomastia and hyperkalemia
Diuretic used to antagonize aldosterone receptors Spironolactone
Antifungal agent used for inhibition of all gonadal and adrenal steroids Ketoconazole
Disease caused by excess ergot alkaloids St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides Autocoids
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 and cimetridine, respectively
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 isoenzyme. 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
Agents for reduction of postpartum bleeding Oxytocin, 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 to treat 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 COX2 COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
Drug that selectively inhibits COX 2 Celecoxib 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 of impotence Alprostadil
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
Methylxanthine derivative used as a remedy for intermittent claudication Pentoxifylline
MOA of corticosteroids inhibit phospholipase A2
SE of long term (>5 days) corticosteroid therapy and remedy Adrenal suppression and weaning slowly, respectively
MOA of penicillin Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
Drug used for MRSA Vancomycin
Vancomycin MOA Blocks cell wall synthesis by sequestration
Genetic basis of low level resistance found with vancomycin Point mutation
Meningitis prophylaxis for persons in contact with patients Ciprofloxacin or Rifampin (for children less than 4 yrs old)
Penicillins active against penicillinase secreting bacteria Methicillin, nafcillin, and dicloxacillin
Cheap wide spectrum antibiotic DOC for otitis media Amoxicillin
Class of antibiotics that have 10% cross sensitivity with penicillins Cephalosporins
PCN active against pseudomonas ceftazidime, imipenem, piperacillin and ticarcillin
Antibiotic causing red-man syndrome, and prevention ancomycin, infusion at a slow rate and antihistamines
Reason fluoroquinolones are contraindicated in children and pregnancy Cartilage damage
Treatment for TB patients (think RIPE ) R ifampin, I soniazid, P yrazinamide, and Ethambutol
Common side effect of Rifampin Red urine discoloration
Cephalosporins able to cross the BBB Ceftazidime, Ceftriaxone or Cefotaxime
Oral 3rd generation cephalosporins NOT able to cross the BBB Cefixime
Drug used for N. gonorrhea in females Ceftriaxone
Cephalosporin causes kernicterus in neonates Ceftriaxone or cefuroxime
SE of imipenem Seizures
Common side effect of hypnotic agents Sedation
Lactams that can be used in PCN allergic patients Aztreonam/carbapenems
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 used to promote sleep Temazpam, trizolam, flurazepam
Benzodiazepine used for anxiety Alprazolam
Non-benzodiazepine used as an anxiolytic Buspirone
Non-benzodiazepine used for sleep Zolpidem
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 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 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
Site of action for zaleplon and zolpidem Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
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
Most frequent route of metabolism Hepatic enzymes
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine Sodium channel 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 for short term (acute) treatment; phenytoin for prolonged therapy
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 origin 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
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 most likely to cause histamine release Tubocurarine
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur Succinylcholine
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine Cholinesterase inhibitors
Facilitates GABA presynaptic inhibition Diazepam
GABA agonist in the spinal cord Baclofen
Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine anal 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 reticulari Amantadine
Inhibitor of MAO type B which slows down metabolism of dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients Selegiline
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's) 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), reserpine
Agents used in Tourette's dx Haloperidol, pimozide , clonidine
Chelating agent used in Wilson's disease Penicillamine
Antipsychotic having the strongest autonomic effects Thioridazine
Example of three antidepressants that are indicated for obsessive compulsive disorder Neurotransmitters affected by the action of antidepressants Clomipramine, fluoxetine and fluvoxamine 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
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
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
Side effects seen with tricyclic antidepressants Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
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 seizues 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
Except for these agents all SSRI have significant inhibition of CytP450 enzyme Citalopram and its metabolite escitalopra
Side effects frequently seen with SSRIs CNS stimulation; GI upset
SSRIs Antidepressants with no effect on BP, no sedation
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx Fluoxetine
SRI indicated for premenstrual dysphoric disorder Fluoxetine (Sarafem)
Some of SSRIs' therapeutic effects beside depression Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrualdysphoric disorder), OCD
SSRI less likely to cause a withdrawal syndrome Fluoxetine
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, used for+A1170 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
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 frequent 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
Prototypical drug is atropine Nonselective Muscarinic Antagonists
Treat manifestations of Parkinson's disease and EPS Benztropine, trihexyphenidyl
Treatment of motion sickness Scopolamine, meclizine
roduce mydriasis and cycloplegia Atropine, homatropine,C1208 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
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; has short duration of action Succinylcholine
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred) Cholinesterase regenerators, pralidoxime
Used to treat patients exposed to insecticides such as parathion Pralidoxime, atropine
This agent cause increased aqueous outflow Prostaglandin PGF2a
These Beta blockers decrease aqueous secretion Timolol (nonselective), betaxolol (selective)
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
Agents that 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
Agents that reduce heart rate, contractility, and O2 * demand Beta-blockers
B-blockers that are more cardioselective beta-1 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
Non-selective Alpha1blockers use to treat pheochromocytoma Phenoxybenzamin
For rebound HTN from rapid clonidine withdrawal Phentolamine
A1a-selective blocker with no effects on HTN 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, and acts centrally 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
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
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
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
SE of thiazide (HCTZ) diuretics Hyperuricemia, hypokalemia and hyperglycemia
Potassium sparing diuretics inhibit Na+/K+ exchange
SE of HMG COA reductase inhibitors Rhabdomyolysis and Hepatotoxicity
Monitoring parameter to obtain before initiation of STATINS LFT's
Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha) Adalimumab, infliximab and etanercept
Created by: tessah10