PHARMACOLOGY I – BLOCK 3:
- General Pharmacology
- Autonomics – PNS
- Autonomics – SNS
- Autonomics – Muscle Relaxants
- Endocrine – Pituitary Hormones
- Endocrine – Diabetes
Q: What clinical trial phase do you test for therapeutic efficacy?
A: Phase II.
Q: What clinical trial phase do you test on 5000 people?
A: Phase III. There are Phases I (25 people/tests safety), II (200 people/tests therapeutic effect), and III (5000 people/compares with other drugs).
Q: Acidic drugs are conjugated to what when excreted?
A: Albumin. Basic drugs bind to glycoprotein.
Q: What’s the only inverse agonist we know?
Q: When rating teratogenicity of a drug, D means…
A: There is evidence of teratogenicity. There is A, B, C, D, and X. A means no teratogenicity. B means no evidence in humans. C means possible teratogenicity. D has evidence. X is contraindicated in pregnancy.
Q: A drug with an abuse potential of I is…
A: highly abusable
Q: What two variables are fixed for drugs?
A: Vd (volume of distribution) and CL (clearance)
Q: What kind of Vd does a drug that stays in the plasma have?
A: Low Vd.
Q: What circulation does a drug go to if it is absorbed through the middle and inferior rectum?
A: Systemic. If superior rectum, goes to portal system.
Q: Conjugation Reaction… is it Phase I or Phase II metabolism?
A: Phase II. Phase I is Microsomal reaction via CYP450 or non-microsomal via XO for allopurinol, MAO, ALDH, etc.
Q: If you have an aspirin overdose (or acidic drug overdose), what do you give to flush away the drug?
A: Anything that would make the urine alkaline — NaHCO3, Potassium Citrate, Acetazolamide
Q: What do you give to flush out a basic drug?
A: anything that would make the urine acidic — Ammonium Chloride, Vitamin C, Cranberry Juice.
Q: Name three substances follow zero-order kinetics?
A: Phenytoin, EtOH, Aspirin
Q: Which type of kinetics is saturable?
A: Zero order kinetics — because the enzyme that breaks down the drug can get saturated.
Q: What is Half Life’s relationship to Volume of Distribution and Clearance?
A: T1/2 = 0.69 Vd/CL
Q: Name the concentration percentages of the first five half lives:
A: 50 –> 75 –> 88 –> 94 –> 97
Q: How many half lives does it take to reach steady state?
A: 5 — up to 97%
Q: How many half lives does it take to reach 90% of steady state?
A: 3.3 half lives
Q: How do you calculate Therapeutic Ratio?
A: Lethal Dose 50 / Effective Dose 50
Q: Two drugs are bioequivalent. What is the maximum possible percent difference between them?
A: 40%. They have same Cmax (peak concentration) and Tmax (time to reach peak concentration)
Q: Which drugs are CYP450 inducers?
A: “Bar Car et Phen Fam” — Barbiturates, Carbamazepine, EtOH, Phenytoin, Rifampin. St. John’s Wort also.
Q: Which drugs are CYP450 inhibitors?
A: “PICK EGS” — Protease Inhibitors, Isoniazid, Cimetidine, Ketonazoles, Erythromycin, Grapefruit Juice, Sulfonamides
Q: Which type of receptors work the fastest?
A: Ion Channel-linked — milliseconds – i.e. Nicotinic Receptor, GABA
G Protein-linked — seconds – i.e. Muscarinic Receptors, Histamine Receptors
Q: Which type of receptors work the slowest?
A: Enzyme-linked receptors — hours — i.e. Cytokine receptors, Tyrosine kinase receptors, other kinase receptors
Intracellular receptors — hours — i.e. Estrogen receptors.
AUTONOMICS — PNS
Q: What gland has muscarinic receptors but is sympathetic?
A: Sweat glands
Q: Butyryl Cholinesterase (Pseudocholine) hydrolyzes what two drugs?
A: Procaine (local anaesthesia), Suxamethonium (muscle relaxant). metabolized in plasma and liver.
Q: M2 receptors are found on…
Q: M1 and M3 works on what signalling pathway?
Q: What organs have both M1 and M3 receptors?
A: GI, Respiratory, Bladder
Q: Ciliary Sphincter vs. Radial Muscle?
A: Ciliary Sphincter innervated by M3 – contraction causes accomodation.
Radial Muscle innervated by A1 – contraction causes mydriasis.
Q: What blood vessels have M3 receptors?
A: vessels used in erection. In all other vessels, sympathetic dominates.
Q: During erection, ACh binds to the M3 on the blood vessels, activating NO Synthase, converting Arginine to NO. What are the steps after this?
A: NO activates Guanyl Cyclase, which converts GTP to cGMP, relaxing the smooth muscle and causing vasodilation of vessels in the penis. KNOW THAT cGMP INCREASES!!!
Q: What blocks SNAP?
A: Botulinum toxin.
Q: What drug treats torticollis?
A: Botulinum toxin. You get torticollis from long-term antipsychotic use.
Q: What drug was used to test for bronchial hypersensitivity?
A: Methacholine (muscarinic agonist). This is called the Methacholine Challenge Test.
Q: What drug treats GI/Bladder Atony?
A: Bethanechol (muscarinic agonist). You give this drug after abdominal surgery in which your bladder and GI are paralyzed.
Q: What’s the antidote for irreversible AChEI poisoning?
A: Pralidoxime (PAM) + Atropine if early. Atropine only if late.
Q: What are the irreversible AChEIs?
A: Organophosphorus insecticides (Parathion, Malathion, Diazinon — “Insects get it ON!”) and Nerve Gases (Soman, Sarin, Tabun)
Q: What site on the acetylcholinesterase do ACh and reversible AChEIs bind to?
A: They bind to both Esteratic Site (more specifically, on the serine of this site) and the Anionic Site.
Q: What site on the acetycholinesterase do irreversible AChEIs bind to?
A: They bind to the Esteratic site only.
Q: What site on the acetylcholinesterase does Pralidoxime bind to?
A: They bind to the Anionic Site, kicking the irreversible AChEI poisons off the esteratic site.
Q: What is it called when the irreversible AChEIs bind to the esteratic site too long and loses alkyl groups to become completely irreversible, and not susceptible to pralidoxime antidote?
A: Aging. Therefore if it’s too late by the time you treat the poison, you give Atropine only, to help with the cardiovascular symptoms and prevent decrease in heart rate or conduction.
Q: What is the Shortest-acting AChEI and what is it used for?
A: Edrophonium (5-15 min), used to diagnose Myasthenia Gravis.
Q: If you wanted to use Edrophonium to treat myasthenia gravis, what other drug do you need to give alongside it?
A: a muscarinic blocker (like atropine), because like carbachol, edrophonium works on both in increasing muscarinic and nicotinic stimulation. Since muscles uses nicotinic, you want to block the muscarinic to prevent decrease in heart rate.
Q: If you have myasthenia crisis, this drug will improve symptoms. If you have cholinergic crisis, it will worsen it. What is it?
A: Edrophonium (AChEI). You get cholinergic crisis from overdose of myasthenia gravis treatment.
Q: Which AChEI is lipid-soluble and crosses membranes and therefore can treat glaucoma?
Q: Which AChEI is water-soluble and does NOT cross membranes and therefore stay in the muscle and can treat myasthenia gravis?
A: Neostigmine, Pyridostigmine.
Q: Hot as a hare, blind as a bat, dry as a bone, red as a beet, and mad as a hatter… What poisoning am I describing?
A: Atropine poisoning — blocks muscarinic, resulting in warm dry skin from decreased sweating/lacrimation/salivation, red from vasodilation, blurry vision from lack of accomodation (ciliary muscle), mad from central nervous effects.
Q: Which anticholinergic drug is used as a preanaesthetic medication to decrease GI and bronchiole secretions before surgery?
Q: What do you use to treat Atropine poisoning?
A: Physostigmine (AChEI) –> increases ACh, counteracting ACh receptor antagonism of atropine.Like atropine (mad as a hatter ), Physostigmine is also lipid-soluble and therefore works (vs. Neostigmine, which is NOT lipid-soluble).
Q: Which anticholinergic drug is used to treat motion sickness?
A: Scopolamine — blocks mainly M1 (CNS), but can block all M1-3.
Q: What’s the anticholinergic drug that works mainly in bronchioles, and therefore used to treat asthma and COPD?
A: Ipratropium. HIGH YIELD!!
Q: What anticholinergic drugs treat overreactive bladder?
A: Oxybutynin, Tolterodine, Darifenacin — all synthetic anticholinergic drugs and stop you from peeing that often. (think of an ox peeing by a tollbooth in Darfur)
Q: Which anticholinergic drug treats IBD?
A: Dicyclomine – works in GI. Antispasmodic.
Q: What M1 antagonists treat Parkinson?
A: Trihexyphenidyl, Benztropine (because a decrease in ACh leads to a decrease in GABA, and therefore an increase in DA, which is what Parkinson patients are lacking).
Q: What drug do you give to recover muscle activity after surgery?
A: Neostigmine – AChEI –> increase ACh –> increase muscle activity. Definitely know this drug for exams.
Q: Which AChEI bind to esteratic site only?
A: All the irreversible ones (insecticides and nerve gases)
Q: What drug causes cycloplegia (can’t accomodate)?
A: Tropicamide, Cyclopentolate — ACh blocked –> no M3 contraction of ciliary sphincter–> can’t accomodate. Think of “Cyclops in the Tropics”
Q: Which muscarinic receptor works via Gi?
A: M2 — hyperpolarize cardiac muscle –> relaxes heart –> decrease HR, conduction
Q: Which cholinergic agonists are not susceptible to AChE?
A: Carbachol and Bethanechol. Remember Carbachol works on both Muscarinic and Nichotinic. Bethanechol is agonist for Muscarinic only and is used after surgeries to bring back GI and bladder tone.
AUTONOMICS — SNS
Q: What kind of G-protein pathway do the following have: A1, A2, B1, B2, M1, M2, M3, D1, D2, H1, H2, V1, V2?
A: qiss qiq siq sqs (“kiss & kick ’til you’re sick of sex”)
Q: What is the only sympathetic receptor that works via Gq?
A: A1 — increase PLC/IP3/DAG –> increase Ca release –> smooth muscle contraction –> peripheral vasoconstriction, contract prostate, constract radial muscles, contract bladder sphincter… you get the point.
Q: What is Dale’s Vasomotor Reversal?
A: It’s when you give an alpha-1 blocker with high-dose epinephrine. It prevents peripheral vasoconstriction, causing blood pressure to go down in high-dose epinephrine (which stimulates B1, A1)
Q: What drug blocks tyrosine hydroxylase (enzyme that makes dopamine from tyrosine)?
A: Metyrosine — decreases DA. treats Pheochromocytoma. Don’t confuse this with Metyrapone which is an adrenal steroid synthesis inhibitor used to treat Cushing’s Syndrome but causes salt and water retention and hirsutism.
Q: Which drugs block NET (NE Transporter)?
A: Cocaine and Imipramine. NE accumulates. Cocaine also blocks DAT (Dopamine Transporter) while Imipramine also increases 5HT. Remember Imipramine is used to treat Panic.
Q: Which drug blocks NE storage in vesicles, preventing its release?
A: Reserpine. Rx Huntingtons
Q: Which drugs promote NE Release?
A: Amphetamine, Ephedrine
Q: What drugs prevented NE release?
A: Bretylium, Guanethidine – Rx HTN
Q: Which MAO breaks down tyramine as well as NE/5HT/DA?
A: MAO-A. MAO-B just does NE/5HT/DA.
Q: MAO-A vs. MAO-B:
A: MAO-A metabolizes NE, 5HT, DA, Tyramine. MAO-B metabolizes NE, 5HT, and DA ONLY. MAO-A works “Anywhere.” MAO-B works on Brain.
Q: What is the cheese effect?
A: Cheese, avocado, beer, and other fermented foods contain tyramine. When you give MAO-A Inhibitors –> tyramine not metabolized –> tyramine go to adrenals and release catecholamines –> hypertensive crisis.
Q: Which MAO-B Inhibitor gives you hepatotoxicity?
A: Rasagiline. The two MAO-B Inhibitors are Rasagiline and Selegiline.
Q: What are the two MAO-A inhibitors?
A: Phenelzine and Tranylcypromine — “Phen and Tran are Maoists”
Q: So MAO-A is found “Anywhere,” and MAO-B is found in the “Brain”… Where is COMT found?
A: Plasma and Liver — sorry don’t have a mnemonic for this one…
Q: Which COMT inhibitor gives you hepatotoxicity?
A: Tolcapone. the other is Entacapone.
Q: What do you use COMT inhibitors for?
A: Rx Parkinson’s Disease.
Q: Which alpha 2 agonist has 100% oral bioavailability
Q: Which drug is practically 100% alpha-1 agonist?
Q: Which sympathomimetic drug gives you rebound hypertension if you miss a dose?
A: Clonidine (alpha-2 agonist, the 100% one). HIGH YIELD!!
Q: What are the only sympathomimetic drugs used to treat hypertension?
A: Clonidine, alpha-methyldopa — because they are alpha-2 agonists.
Q: What is the drug of choice for pregnancy-induced hypertension?
A: Alpha-methyldopa — alpha-2 agonist. Think of it as “alpha-mother-dopa.”
Q: Which sympathomimetic drug is both beta-1 and 2 agonist?
A: isoproterenol aka isoprenaline
Q: Which sympathomimetic drug is a dopamine analogue that doesn’t bind dopamine receptors?
A: Dobutamine — instead it is a beta-1 agonist.
Q: Which sympathomimetic drug is the preferred treatment for Heart Failure?
A: Dobutamine — beta-1 agonist — because it increases contraction force in the heart without increasing HR (because also stim beta-2 –> dilate muscle vessels –> preventing increase in HR)
Q: How does the drug of choice of Asthma work?
A: Albuterol — beta 2 agonist –> dilates bronchioles, breathe better.
Q: What sympathomimetic drug is a D1 agonist, and therefore increase renal blood flow –> decreased renin –> decreased ATII –> decreased vasoconstriction –> vasodilation, and therefore good to treat Emergency Hypertension?
A: Fenoldopam – “Fenol-D1-pam.” KNOW THIS!!
Q: Which indirectly-acting adrenergic agonist activates the Radicular Activating System (RAS), keeping you awake, and therefore good for treating Narcolepsy, and increases your focus in ADHD?
A: Amphetamine — it is indirectly-acting because it increases NE and DA release, rather than directly bind to sympathetic receptors.
Q: What drug is a mixed adrenergic agonist?
A: Ephedrine — direct agonist of A1 A2 B1 B2. Indirectly increase NE release.
Q: Epinephrine at high dose bind what receptors?
A: B1, B2, A1 (constrict peripheral vessels –> increase BP)
Q: Epinephrine at low dose bind what receptors?
A: B1, B2 (dilate muscle vessels –> decrease BP)
Q: Compare ocular symptoms of Atropine and Epinephrine:
A: Atropine: mydriasis, No Accomodation (because block M3 and other muscarinics)
Epinephrine: mydriasis, Accomodation Normal (nothing to do with M3)
Q: Who do you not use Norepinephrine with?
A: Asthma patients. Why would you? There’s no B2 action!
Q: How does Amphetamine increase DA release?
A: they block VMAT –> DA can’t go into vesicles –> DA accumulates inside cell –> DAT reverses direction –> DA flow out.
Q: Which drugs give reflex bradycardia?
A: alpha 1 agonist (phenylephrine, mephenteramine, methoxamine), Norepinephrine, and really high dose Epinephrine (but on test, don’t assume epinephrine will have reflex bradycardia)
Q: What adrenergic receptor increases PP/HR?
Q: What adrenergic receptor increases BP/TPR?
A: A1 (because constrict peripheral vessels)
Q: What adrenergic receptor decreases BP/TPR?
A: B2 (because dilate skeletal muscle vessels)
Q: Dopamine at low dose bind what receptors?
A: D2, D1 (renal vasodilation –> increase urine)
Q: Dopamine at medium dose bind what receptors?
A: D2, B1 (increase heart contraction)
Q: Dopamine at large dose bind what receptors?
A: D2, A1 (peripheral vasoconstriction –> increase BP)
Q: What drug stops preterm labor?
A: Ritodrine — B2 agonist –> relaxes uterus.Also induce maturation of lungs in premature baby.
Q: What adrenergic receptor causes increase in aqueous humor production?
A: B2 — remember Sub SLC. C = ciliary epithelium, which makes aqueous humor.
Q: Which drugs will give you postural hypotension as a first dose phenomenon?
A: Alpha-1 selective blockers — Prazosin, Terazosin, Doxazosin, Tamsulosin — all the zosin’s
Q: Which alpha blocker can you treat pheochromocytoma?
A: Phenoxybenzamine (irreversible, non-selective) — Nowadays, you would use both alpha and beta blocker at the same time, because if you just block alpha receptors, the NE can still work on B1, which can increase HR and cause hypertension. See labetalol and carvedilol.
Q: Which alpha blockers are non-selective, REVERSIBLE?
A: Phentolamine, tolazoline
Q: Which alpha blockers are non-selective, IRREVERSIBLE?
Q: Which alpha blocker is used to treat Erectile Dysfunction?
A: Yohimbine… because it is an alpha-2 selective blocker, which does negative feedback on sympathetic –> increased sympathetic –> ejaculation.
Q: Which drug is alpha-2 selective blocker?
Q: What drugs block both A1 and B?
A: Labetalol and Carvedilol… therefore treat pheochromocytoma.
Q: Which B1 blocker crosses BBB?
Q: Which B1 blocker is the shortest acting?
Q: Which B1 blocker has intrinsic activity/partial agonist?
Q: Which non-selective B blocker has intrinsic activity/partial agonist?
Q: What drugs do you not give diabetes because it blocks their “hypoglycemic warning sign” as well as block glycolysis during hypoglycemia?
A: beta-blockers. hypoglycemia will normally cause fight or flight response to increase glycolysis (B2 action), and doing so, also causes tachycardia (B1 action) which give diabetics a warning. If you give a beta-blocker, you block both of the mechanism of “salvation” and mechanism of “warning,” particularly with drugs that block both B1 and B2 like Propranolol, Nadolol, Timolol, Pindolol, Labetalol, or Carvedilol.
Q: What sympathetic blocker do you NOT use in asthma?
A: the non-selective beta blockers, because they block B2, so your bronchioles can’t dilate.
AUTONOMICS — MUSCLE RELAXANTS
Q: Which drug is the DOC for Malignant HTN?
A: Dantrolene (directly acts on Ca channels), like Malignant HTN caused by Succinylcholine.
Q: What alpha-2 agonist is used as a centrally-acting muscle relaxant?
Q: Which type of muscle relaxants are reversed by neostigmine?
A: Non-depolarizing ones, because they are competitive.
Q: Why do you give muscle relaxants via IV?
A: Because they do not cross membranes or BBB — only go to muscle.
Q: What is the shortest acting non-depolarizing muscle relaxant?
Q: What are the longest acting non-depolarizing muscle relaxants?
A: Pancuronium and Pipecuronium — “Long Pan-Pipe”
Q: Which non-depolarizing muscle relaxant muscle relaxant undergoes spontaneous, non-enzymatic degradation (Hoffman Elimination), NOT kidney or liver?
A: Cisatracurium — intermediate acting
Q: Which Non-depolarizing muscle relaxants are intermediate acting?
A: Rocuronium (know this one), Vecuronium, Cisatracurium.
Q: Which muscle relaxant causes Malignant Hyperthermia?
Q: Which muscle relaxant do you NOT give people who already have muscle damage (like those who had car accidents)?
A: Succinylcholine — because they are already hyperkalemic. Succinylcholine makes them even more hyperkalemic. Can lead to arrhythmias. Both Hypo and Hyperkalemia can lead to arrhythmias.
Q: Which muscle relaxant can cause apnea if you are pseudocholinesterase deficient?
Q: Which muscle relaxant can give you initial fasciculations?
A: Succinylcholine — because it depolarizes.
Q: Which muscle relaxant acts directly on Ryanodine receptors?
Q: What are the Centrally-acting muscle relaxants?
A: Methocarbamol, Chlorzoxazone, Diazepam, Baclofen, Tizanidine
Q: Which muscle relaxant increases GABA-A action?
A: Diazepam. Remember GABA blocks DA release in brain.
Q: Which muscle relaxant increases GABA-B action?
Q: What can you use to treat dissecting aortic aneurysm?
A: Ganglion Blockers
Q: What kind of drugs block reflex bradycardia or tachycardia?
A: Ganglion Blockers
Q: What drugs reverse the predominant autonomic tone in organs?
A: Ganglion blockers. Therefore, for vessels, since the predominant tone is sympathetic, ganglion blockers will cause the opposite — parasympathetic effect, causing vasodilation and hypotension.
ENDOCRINE — PITUITARY HORMONES
Q: What drug treats acromegaly, refractory diarrhea, and esophageal varices?
A: Octreotide — short acting somatostatin analog
Q: What endocrine drug is good to treat acromegaly but not necessarily refractory diarrhea or esophageal varices?
A: Lanreotide — because it is a long-acting somatostatin analogue.
Q: What drug is used to diagnose congenital adrenal hyperplasia?
A: Cosyntropin, an ACTH analogue
Q: What acromegaly drug is a GH receptor antagonist?
Q: Which drug is both an FSH and LH analogue?
Q: Which acromegaly drug gives you gallstones?
A: octreotide, because it mimics somatostatin and slows bile flow.
Q: Which dopamine agonists can you use to treat acromegaly?
A: Cabergoline, Bromocriptine
Q: Patient comes in with Galactorrhea and Infertility after taking antipsychotic drugs. What do you use to treat?
A: Cabergoline and Bromocriptine. They are DA Agonists. Patient has Hyperprolactinoma
Q: What drug prevents preterm labor?
A: Atosiban, an oxytocin antagonist.
Q: What drug do you use to prevent postpartum hemorrhage and induce labor?
A: Oxytocin — contracts uterus –> compress vessels –> stops bleeding.
Q: What drug is contraindicated in Fetal distress, Cephalopelvic Disproportion, and Prematurity?
A: Oxytocin — because crosses placenta, you don’t want to give fetus tachycardia. You don’t want to force labor when mother’s pelvis too small, and you don’t want to force labor when the baby’s not ready to come out yet.
Q: What is the adverse effect of Oxytocin?
Q: Vasopressin binds to V1 and V2 receptors. What do they do?
A: V1 — vasoconstriction. V2 — inserts aquaporins in renal collecting ducts –> water retention. Both of these actions, of course, increases blood pressure.
Q: Which ADH agonist treats central diabetes insipidus?
Q: Which drug do you use to treat nocturnal enuresis?
A: Desmopressin, an AVP/ADH agonist –> water retention
Q: Which endocrine drug can be used to treat hemophilia and von Willebrand Disease?
A: Desmopressin, because AVP/ADH also release factors VIII and vWF.
Q: Which drugs can indirectly cause water retention (and therefore treat Central Diabetes Insipidus) by stimulating AVP/ADH?
A: NSAIDs, Carbamazepine, Chlorpropamide
Q: Which drugs can give you Diabetes Insipidus because it inhibits AVP/ADH?
A: Demeclocycline, Lithium, Conivaptan/Tolvaptan (ADH antagonists)
Q: What drugs can you use to treat Nephrogenic Diabetes Insipidus?
A: Amiloride (if NDI is Li-induced), Thiazide (if NDI is NOT Li-induced), Indomethacin, Water.
Q: Which drugs treat SIADH?
A: Conivaptan and Tolvaptan — ADH antagonists.
Q: Which GnRH analogue is short acting?
A: Gonadorelin — so you can use in pulses to induce fertility.
Q: Which GnRH analogue is long acting?
A: Leuprolide, Nafarelin, and Goserelin — therefore you can give in continuous dose to inhibit gonadotropin release (but since it’s an analogue, it will have initial transient increased release), Rx prostate cancer, endometriosis.
Q: What drug is used to distinguish Cushing’s Syndrome from ectopic ACTH secretion?
A: Corticorelin — a CRH analogue
Q: What drug is a GHRH analogue?
Q: What drug is a TRH analogue?
Q: Which drug is an GnRH Antagonist?
A: Ganirlix, Cetrorelix
Q: Which drug treats Laron Dwarfism?
A: Mecasermin — recombinant IGF-1. Patients are GH-insensitive, leading to dwarfism.
Q: Which drug causes cancer, carpal tunnel syndrome, and pseudotumor cerebri?
ENDOCRINE — DIABETES
Q: Which organs do not depend on insulin to get glucose?
A: Nerves, RBC, Kidney, and Lens
Q: Patient comes in with Diabetes and Pregnancy. What drug do you use?
A: Regular Insulin
Q: Which type of insulin treats ketoacidosis?
A: Regular insulin
Q: Which insulins are intermediate acting?
A: Neutral Protamine Hagedorn (NPH) and Lente
Q: Which insulins are long-acting, creating a basal level?
A: Ultralente, Glargine, and Detimir.
Q: Which diabetes drug causes SIADH-like adverse effects?
A: Chlorpropamide, a sulfonylureas. Increase ADH.
Q: What is the most potent sulfonylurea?
A: Glimiperide, third generation
Q: Which insulin secretagogues do you take with each meal?
A: Repaglinide, Nateglinide, Meglitinide — because shorter acting.
Q: Which oral diabetes drug is known to cause hypoglycemia and weight gain?
A: Sulfonylureas. In contrast, the other insulin secretagogues (Repaglinide, Meglitinide, and Nateglinide) are more rapid, short-acting, has less weight gain and less hypoglycemia than sulfonylureas.
Q: Which drugs do you use to treat Diabetes with impaired renal function?
A: Repaglinide, Nateglinide, Meglitinide — they are insulin secretagogues that have MINIMAL RENAL EXCRETION.
Q: Which diabetes drug does not cause hypoglycemia?
A: Biguanides (Metformin) because it just decreases gluconeogenesis.
Q: Which diabetes drug should you NOT use with kidney or liver impairment, or alcohol consumption?
A: Metformin, because they can cause additional lactic acidosis.
Q: Which drugs increases your GLUT-4?
A: Thiazolidinediones (Pioglitazone, Rosiglitazone, Troglitazone) — increase tissue sensitivity to insulin. “Pio, Rosi, and Trog”
Q: Which drugs are PPAR-gamma agonists?
A: Thiazolidinediones (Pioglitazone, Rosiglitazone, Troglitazone) — increase tissue sensitivity to insulin. Rx Diabetes.
Q: Which thiazolidinedione gives you hepatitis, and therefore is no longer used?
Q: Which diabetes drug gives you diarrhea and flatulence?
A: Acarbose and Miglitol — alpha-glucosidase inhibitors — inhibit breakdown of carbs.
Q: Which diabetes drug is a GLP-1 analogue?
A: Exenatide. It is an incretin –> decreases glucagon release, increases insulin after meals.
Q: Which diabetes drug do you use only as an adjunct?
A: Pramlintide — because it’s an amylin analogue, which is an adjuct co-released with insulin. Slows gastric emptying
Q: What can you use to treat beta-blocker overdose?
A: Glucagon, because it increases inotropy and chronotropy of heart, without needing to bind the beta-1 receptors (but instead bind glucagon receptors)
Q: Which oral antidiabetic drug has disulfiram-like reaction?
A: Sulfonylureas (“AC Tol Tol, Glip Glyb, and Glim”)
Q: What’s the drug of choice for Type II Diabetes?
A: Metformin — because it does not cause hypoglycemia. It also gives you weight loss, just in case you are obese
Q: Which type of oral antidiabetic drug blocks potassium channels?
A: Sulfonylureas. It blocks K channels –> K can’t go out of cell –> membrane depolarizes –> calcium enters –> insulin released.
Q: Which two types of drugs are insulin sparing (meaning they don’t use insulin at all, and therefore prevents development of insulin resistance)?
A: Biguanides (Metformin, which decrease gluconeogenesis), alpha glucosidase inhibitors (Acarbose, Miglitol, which inhibit breakdown of carbs)
Q: What drug inhibits DPP-4 so you can’t inactivate incretin and therefore increase insulin release after meals?