Pharm USMLE 2 Flashcards
What is the specific clinical use of Indomethacin in neonates?
Indomethacin is used to close a patent ductus arteriosus.
What is used to reverse the action of Heparin?
Protamine Sulfate is used for rapid reversal of heparinization (positively charged molecule that binds to negatively charged heparin).
What patients are at risk for life threatening hypotension when taking Sildenafil (Viagra)?
Those patients who are taking nitrates.
What process does Zafirlukast interfere with?
Leukotrienes increasing bronchial tone.
What type of gout is treated with Allopurinol?
Chronic gout.
What type of gout is treated with Colchicine?
Acute gout.
What type of gout is treated with Probenacid?
Chronic gout.
What type of patient should not take Misoprostol and why?
Misoprostol is contraindicated in women of childbearing potential because it is an abortifacient.
Which H2 Blocker has the most toxic effects and what are they?
Cimetidine is a potent inhibitor of P450; it also has an antiandrogenic effect and decreases renal excretion of creatinine. Other H2 blockers are relatively free of these effects.
Why are the Sulfonylureas inactive in IDDM (type-1)?
Because they require some residual islet function.
Acetaldehyde is metabolized by Acetaldehyde dehydrogenase, which drug inhibs this enzyme?
-Disulfram & also sulfonylureas, metronidazole
Explain pH dependent urinary drug elimination?
-Weak Acids>Alkinalize urine(CO3) to remove more -Weak bases>acidify urine to remove more
How do you treat coma in the ER (4)?
-Airway -Breathing -Circulation -Dextrose (thiamine & narcan) -ABCD
In coma situations you rule out what (7)?
-Infections -Trauma -Seizures -CO -Overdose -Metabolic -Alcohol (IT’S COMA)
List some specifics of lead poisoning(4)?
-A57Blue lines in gingiva & long bones -Encephalopathy & Foot drop -Abdominal colic / -Sideroblastic anemia
List the specific antidote for this toxin: Acetaminophen
-N-acetylcystine
List the specific antidote for this toxin: Amphetamine
-Ammonium Chloride
List the specific antidote for this toxin: Anticholinesterases (organophosphate.)
-Atropine & pralidoxime
List the specific antidote for this toxin: Antimuscarinic (anticholinergic)
-Physostigmine salicylate
List the specific antidote for this toxin: Arsenic (all heavy metals)
-Dimercaprol, succimer
List the specific antidote for this toxin: Benzodiazepines
-Flumazenil
List the specific antidote for this toxin: Beta Blockers
-Glucagon
List the specific antidote for this toxin: Carbon monoxide
-100% oxygen, hyperbaric
List the specific antidote for this toxin: Copper
-Penicillamine
List the specific antidote for this toxin: Cyanide
-Nitrate, hydroxocobalamin thiosulfate
List the specific antidote for this toxin: Digitalis
-Normalize K+, Lidocaine, & Anti-dig Mab
List the specific antidote for this toxin: Heparin
-Protamine
List the specific antidote for this toxin: Iron
-Deferoxamine
List the specific antidote for this toxin: Lead
-EDTA, dimercaprol, succimer, & penicillamine
List the specific antidote for this toxin: Methanol & Ethylene glycol
-Ethanol, dialysis, & fomepizole
List the specific antidote for this toxin: Methemoglobin
-Methylene blue
List the specific antidote for this toxin: Opioids
-B51Naloxone / naltrexone (narcan)
List the specific antidote for this toxin: Salicylates
-Alkalinize urine & dialysis
List the specific antidote for this toxin: TPA & Streptokinase
-Aminocaproic acid
List the specific antidote for this toxin: Tricyclic antidepressants
-NaHCO3
List the specific antidote for this toxin: Warfarin
-Vitamin K & fresh frozen plasma
What are the products and their toxicities of the metabolism of ethanol by / alcohol dehydrogenase?
-Acetaldehyde -Nausea, vomiting, headache, & hypotension
What are the products and their toxicities of the metabolism of Ethylene Glycol by / alcohol dehydrogenase?
-Oxalic acid -Acidosis & Nephrotoxicity
What are the products and their toxicities of the metabolism of Methanol by / alcohol dehydrogenase?
-Formaldehyde & formic acid -severe Acidosis & retinal damage
Which drug(s) cause this reaction: Adrenocortical Insufficiency
-Glucocorticoid withdrawal
Which drug(s) cause this reaction: Agranulocytosis (3)?
-Cloazapine -carbamazapine -colchicine -PTU
Which drug(s) cause this reaction: Anaphylaxis?
-penicillin
Which drug(s) cause this reaction: Aplastic anemia (5)?
-Chloramphenicol -benzene -NSAIDS -PTU -phenytoin
Which drug(s) cause this reaction: Atropine-like side effects?
-Tricyclic antidepressants
Which drug(s) cause this reaction: Cardiac toxicity?
-Daunorubicin & Doxorubicin
Which drug(s) cause this reaction: Cinchonism (2)?
-Quinidine -quinine
Which drug(s) cause this reaction: Cough?
-ACE inhibitors (Losartan>no cough)
Which drug(s) cause this reaction: Cutaneous flushing (4)?
-Niacin -CA++ channel blockers -adenosine -vancomycin
Which drug(s) cause this reaction: Diabetes insipidus?
-Lithium
Which drug(s) cause this reaction: Disulfram-like reaction (4) ?
-metronidazole -certain cephalosporins -procarbazine -sulfonylureas
Which drug(s) cause this reaction: Drug induced Parkinson’s (4) ?
-Haloperidol -chlorpromazine -reserpine -MPTP
Which drug(s) cause this reaction: Extrapyramidal side effects (3)?
-chlorpromazine -thioridazine -Haloperidol
Which drug(s) cause this reaction: Fanconi’s syndrome?
-Tetracycline
Which drug(s) cause this reaction: Focal to massive hepatic necrosis (4)?
-Halothane -Valproic acid -acetaminophen -Amantia phalloides
Which drug(s) cause this reaction: G6PD hemolysis(8)?
-Sulfonamides -INH -ASA -Ibuprofen -primaquine -nitrofurantoin /-pyrimethamine -Chloramphenicol
Which drug(s) cause this reaction: Gingival hyperplasia?
-phenytoin
Which drug(s) cause this reaction: Gray baby syndrome?
-Chloramphenicol
Which drug(s) cause this reaction: Gynecomastia (6)?
-Cimetidine -ketoconazole -spironolactone -digitalis -EtOH -estrogens
Which drug(s) cause this reaction: Hepatitis?
-Isoniazid
Which drug(s) cause this reaction: Hot flashes?
-Tamoxifen
Which drug(s) cause this reaction: Neuro and Nephrotoxic?
-polymyxins
Which drug(s) cause this reaction: Osteoporosis (2)?
-Corticosteroids -heparin
Which drug(s) cause this reaction: Oto and Nephrotoxicity (3)?
-aminoglycosides -loop diuretics -cisplatin
Which drug(s) cause this reaction: P450 induction(6)?
-Barbiturates -phenytoin -carbamazipine -rifampin -griseofulvin -Quinidine
Which drug(s) cause this reaction: P450 inhibition(6)?
-Cimetidine -ketoconazole -grapefruit juice -erythromycin -INH -Sulfonamides
Which drug(s) cause this reaction: Photosensitivity(3)?
-Tetracycline -amiodarone -Sulfonamides
Which drug(s) cause this reaction: Pseudomembranous colitis?
-Clindamycin
Which drug(s) cause this reaction: Pulmonary fibrosis(3)?
-Bleomycin -amiodarone -busulfan
Which drug(s) cause this reaction: SLE-like syndrome?
-Hydralazine -Procainamide -INH -phenytoin
Which drug(s) cause this reaction: Stevens-Johnson syn. (3)?
-Ethosuxamide -Sulfonamides -lamotrigine
Which drug(s) cause this reaction: Tardive dyskinesia?
-Antipsychotics
Which drug(s) cause this reaction: Tendonitis and rupture?
-Fluoroquinolones
Which drug(s) cause this reaction: Thrombotic complications?
-Oral Contraceptives
Which drug(s) cause this reaction: Torsade de pointes (2)?
-Class III antiarrhythmics (sotalol) -Class IA (Quinidine)
Which drug(s) cause this reaction: Tubulointerstitial Nephritis (5)?
-Sulfonamides -furosemide -methicillin -rifampin -NSAIDS (ex. ASA)
Describe first-order kinetics?
Constant FRACTION eliminated per unit time.(exponential)
Describe Phase I metabolism in liver(3)?
-reduction, oxy, & hydrolysis -H2O sol. Polar product -P450
Describe Phase II metabolism in liver(3)?
-acetylation, glucuron., & sulfation -Conjugation -Polar product
Explain differences between full and partial agonists(2).
- Act on same receptor - Full has greater efficacy
Explain potency in relation to full and partial agonists(2).
- partial agonist can have increased, decreased, /A21or equal potency as full agonist. - Potency is an independent factor.
How do spare receptors effect the Km?
- ED 50 is less than the Km (less than 50% of receptors)
How do you calculate maintenance dose?
Md’ (CpxCL)/F Cp’ plas. Conc. CL’clear. F’bioaval.
How does a competitive antagonist effect an agonist?
-Shifts the curve to the right -increases Km
How does a noncompetitive antagonist effect an agonist?
- Shifts the curve down -reduces Vmax
Name the steps in drug approval(4)?
-phase I (clinical tests) -phase II -phase III -PhaseIV (surveillance)
Steady state concentration is reached in __ number of half-lifes
In 4 half-lifes’ (94%) T1/2 ‘ (0.7x Vd)/CL
What is the definition of zero-order kinetics? Example?
-Constant AMOUNT eliminated per unit time. -EtOH & ASA
What is the formula for Clearance (CL)
CL’ (rate of elimination of drug/ Plasma drug conc.)
What is the formula for Volume of distribution (Vd)
Vd’ (Amt. of drug in body/ Plasma drug conc.)
What is the loading dose formula?
Ld’ (CpxVd)/F Cp’plasma conc. F’ Bioaval.
A 12yo patient was treated for a reaction to a bee sting, what drug provides the best coverage of sympathomimetic receptors?
Epinephirine(Alpha1,2 and Beta 1,2)
A 57 yo heart failure pt develops cardiac decompensation, what drug will give you adequate perfusion of his kidneys as well as tx for his Hypotension
Dopamine
A fellow passenger on a Carnival cruise ship looks pale and diaphoretic, what antimuscarinic agent would you give them?
scopolamine
A group of pts are rushed into the ER complaining of excessive sweating, tearing, salivation, HA, N and V, muscle twitching, difficulty breathing and diarrhea. What drug would be the most effective immediate tx
Atropine pts are suffering from Cholinestrase inhibitor poisining (Nerve gas/Organophosphate poisining)
As an Anes you want to use a depolarizing neuromuscular blocking drug on your pt, what do you use
Succinylcholine
MOA of Succinylcholine
Prevents the release of Ca from SR of skeletal muscle
Clonidine is the preferred sym pathomimetic tx of HTN in pts with renal disease, why??
Centrally acting alpha agonist, thus causing a decrease in central adrenergic outflow, spairing renal blood flow
Cocaine casues vasoconstriction and local anesthesia by what mechanism
Indirect agonist, uptake inhibitor
Cocaine shares is mechanism of action with what antidepressant
TCA
Dobutamine used for the tx of shock acts on which receptors
Beta1 more than B2
Guanethidine enhances the release of Norepi?
No, it inhibits the release of Nor Epi
How does angiotensin II affect NE release?
It acts presynaptically to increase NE release.
How does botulinum toxin result in respiratory arrest?
Prevents the release of ACh, which results in muscle paralysis.
How does dantrolene work?
Prevents the release of calcium from the sarcoplasmic reticulum of skeletal muscle.
How does NE modulate its own release? What other neurotransmitter has this same effect?
NE acts presynaptically on alpha-2 receptors to inhibit its own release. ACh also acts presynaptically through M1 receptors to inhibit NE release.
How would hemicholinium treatment affect cholinergic neurons?
Hemicholinium inhibits the transport of choline into the nerve, thus inhibiting formation of ACh.
How would you reverse the effect of a neuromuscular blocking agent?
Give an antichloinesterase - neostigmine, edrophonium, etc
If a patient is given hexamethonium, what would happen to his/her heart rate?
It would increase to ~ 100 beats/min. Both sympathetic and vagal stimulation would be knocked out, but the SA node has an intrinsic pace of 100 beats/min, which is normally checked by vagal stimulation.
Isopoterenol was given to a patient with a developing AV block, why?
Stimulates beta adrenergic receptors
Norepi feedbacks and inhibits the presynaptic receptor by what mechanism
Binding to the presynaptic alpha 2 release modulating receptors
Reserpine will block the syntheis of this drug and but not its precursor.
Blocks Norepi, but not Dopamine
These drugs acts indirectly by releasing strored catecholamines in the presynaptic terminal
Amphetamine and Ephedrine
What anticholinesterase crosses the blood-brain-barrier?
physostigmine
What antimuscarinic agent is used in asthma and COPD?
Ipratropium
What antimuscarinic drug is useful for the tx of asthma
Ipratropium
What are the classic symptoms of cholinesterase inhibitor poisoning (parathion or other organophosphates)?
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation ‘ DUMBBELS; also abdominal cramping
What are the clinical indications for bethanechol?
Activates cholinergic receptors on bladder and bowel smooth muscle, alleviating post-op and neurogenic ileus and urinary retention.
What are the clinical indications for neostigmine?
Post-op and neurogenic ileus and urinary retention, myasthenia gravis, and reversal of neuromuscular junction blockade (post-op) through anticholinesterase activity.
What are the indications for using amphetamine?
narcolepsy, obesity, and attention deficit disorder (I wouldn’t recommend this)
What are the nondepolarizing neuromuscular blocking drugs?
Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rapacuronium
What are the phases of succinylcholine neuromuscular blockade?
Phase 1 ‘ prolonged depolarization, no antidote, effect potentiated by anticholinesterase; Phase 2 ‘ repolarized but blocked, an anticholinesterase is the antidote for this phase.
What are two indirect acting adrenergic agonists?
amphetamine and ephedrine
What beta 2 agonist will help your 21yo Astma pt?
Albuterol, tertbutaline
What cholinergic inhibitor acts by directly inhibiting Ach release at the presynaptic terminal
Botulinum
What cholinomimetic is useful in the diagnosis of Myasthenia Gravis
Edrophonium
What cholinomimetics might your pt be taking for his glaucoma
Carbachol, pilocarpine, physostigmine, echothiophate
What class of drug is echothiophate? What is its indication?
anticholinesterase glaucoma
What conditions would you use dantrolene?
In treatment of malignant hyperthermia, due to concomitant use of halothane and succinylcholine. Also in neuroleptic malignant syndrome, a toxicity of antipsychotic drugs.
What drug is used to diagnose myasthenia gravis?
edrophonium (extremely short acting anticholinesterase)
What drugs target anticholinesterase
Neostigmine, pyridostigmine edrophonium, physostigmine echothiophate
What effect would atropine have on a patient with peptic ulcer disease?
Theoretically it could be used to block the cephalic phase of acid secretion (vagal stimulation).
What effect would atropine have on the preganglionic sympathetic activation of sweat glands? Would this person sweat?
None. No, because atropine would block the postganglionic muscarinic receptors involved in sweat gland stimulation.
What enzyme is responsible for the breakdown of ACh in the synaptic cleft?
Acetylcholinesterase; ACh is broken down into choline and acetate.
What enzyme is responsible for the degredation of Ach
Acetylcholine esterase
What enzyme is responsible for the production of Ach from Acetyl CoA and Choline
Choline acetyltransferase
What is the clinical utility of clonidine?
Treatment of hypertension, especially with renal disease (lowers bp centrally, so flow is maintained to kidney).
What is the clinical utility of cocaine?
The only local anesthetic with vasoconstrictive properties.
What is the difference between the affinity for beta receptors between albuterol/terbutaline and dantroline?
Dobutamine has more of an affintiy for beta-1 than beta-2, and is used for treating heart failure and shock. Albuterol and terbutaline is the reverse, and is used in treatment of acute asthma.
What is the difference in receptor affinity of epinephrine at low doses? High doses?
Prefers beta’s at low doses, but at higher doses alpha agonist effects are predominantly seen.
What is the effect of epinephrine infusion on bp and pulse pressure?
Increased systolic and pulse pressure, decreased diastolic pressure, and little change in mean pressure.
What is the effect of guanethidine on adrenergic NE release?
It inhibits release of NE.
What is the effect of norepinephrine on bp and pulse pressure?
Increases mean, systolic, and diastolic bp, while there is little change in pulse pressure.
What is the effect of TCA’s on the adrenergic nerve?
They inhibit reuptake of NE at the nerve terminal (as does cocaine).
What is the only depolarizing neuromuscular blocking agent?
Succinylcholine
What is the receptor affinity and clinical use of isoproterenol?
It affects beta receptors equally and is used in AV heart block (rare).
What physiological effects was the Anes using Atropine to tx
SLUD (salivation, Lacrimation, urination, Defecation)as well as airway secretion, GI motility, acid secretions
What reversal agent could a Anes give to reverse the effects of Atropine
Bethanechol, Neostigmine, physostigmine
What side effect of using atropine to induce pupillary dilation would you expect?
Atropine would also block the receptors in the ciliary muscle, causing an impairment in accommodation (cycloplegia).
What sympathomimetic would you not prescribe for hypotension in a pt with renal artery sclerosis.
Norepinephrine (Alpha1,2 and beta 1)
What type of neurological blockade would hexamethonium create?
Hexamethonium is a nicotinic antagonist, and thus is a ganglionic blocker.
What would be the effect on blood pressure with infusion of the alpha -2 agonist clonidine?
Initially vasoconstriction would increase bp, but then it acts on central alpha-2 receptors to decrease adrenergic outflow resulting in decreased bp.
Which antimuscarinic agents are used in producing mydriasis and cycloplegia?
atropine, homatropine, tropicamide
Which drug increases Sys BP w/o affecting Pulse Pressure
Epinephrine
Which of epi, norepi, or isoproterenol results in bradycardia?
Norepinephrine
Which of the following would atropine administration cause? Hypothermia, bradycardia, excess salivation, dry flushed skin, or diarrhea
Dry flushed skin, due to inhibition of sympathetic post-ganglionic blockade on muscarinic receptors of sweat glands. All others are opposite of what would be expected.
Which of these three drugs will cause a reflex bradycardia in your pt (Norepi, Epi, or Isoporterenol)
Norepinephrine
Which receptors does phenylephrine act upon?
alpha-1 > alpha-2; used as a pupil dilator, vasoconstrictor, and for nasal decongestion
While at a tail gait party, you bite into a sandwich that a yellow jacket is also enjoying. Knowing your allergy to this creature, what should you do?
Epinephrine to treat anaphylaxis. Also useful if you have open angle glaucoma, asthma, or hypotension.
Why are albuterol and terbutaline effective in tx of acute asthmatic attacks?
These B-2 agonists cause respiratory smooth muscle to relax.
Why does atropine dilate the pupil?
Blocking muscarinic receptors in the circular fibers of the eye, results in unopposed action of radial muscles to dilate.
Why does NE result in bradycardia?
NE increases bp, which stimulates baroreceptors in the carotid sinus and the aorta. The CNS signals through vagal stimulation to decrease heart rate.
Why is carbachol and pilocarpine useful in treatment of glaucoma?
They activate the ciliary muscle of the eye (open angle) and pupillary sphincter (narrow angle).
Why is pyridostigmine effective in the treatment of myasthenia gravis?
As an anticholinesterase it increases endogenous ACh and thus increases strength.
Why is reserpine effective in treating HTN?
Reserpine inhibits dopamine transport into vesicles, attenuating its conversion to NE by dopamine beta-hydroxylase.
Why is there a drop in systolic, mean, and diastolic bp with infusion of isoproterenol?
Stimulating beta receptors stimulates heart rate, but beta receptor induced vasodilation reduces peripheral resistance.
Why would a patient with cog-wheel rigidity and a shuffling gait be given benztropine?
Parkinson patients benefit from antimuscarinic agents through its inhibitory action within the indirect pathway.
Why would dopamine be useful in treating shock?
Receptors ‘ D1’D2>beta>alpha, thus increasing heart rate (beta) and blood pressure (alpha vasoconstriction) while maintaining kidney perfusion (dopamine receptors)
Why would you give a drug like pancuronium or succinylcholine?
Useful in muscle paralysis during surgery or mechanical ventilation.
Why would you use pralidoxime after exposure to an organophosphate?
Pralidoxime regenerates active cholinesterase.
Will Hemicholinum affect the release of stored Ach during Cholinergic Stimulation
No, hemicholinum block the uptake of Choline and thus Ach synthesis
Would blockade of muscarininc receptors in the bladder be useful in treating urinary retention?
No. Atropine is used to reduce urgency in mild cystitis. So it would aggravate the urinary retention.
Your patient wants an effective drug to treat his motion sickness, what would you prescribe
Scopolamine
Abciximab, Tirofiban, Eptifibatide – MOA?
Glycoprotein IIb/IIIa inhibitors (inhibit platelet binding w/ fibrinogen & fibronectin)
Abciximab, Tirofiban, Eptifibatide – Clinical use(s)?
Following percutaneous intervention (PCI) in acute coronary syndrome
Argatroban – MOA?
Direct Thrombin Inhibitor (DTI)
– used following Heparin-Induced Thrombocytopenia
