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Combined Rx
Pharmacology One-lIners
Question | Answer |
---|---|
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 |