Drugs Flashcards
Learn to spell out drugs
What drug is a first line TB treatment and causes increased nerologic side effects in pts with NAT-2 polymorphism?
isoniazid
What drug causes excessive hypotension along with CYP2D6 polymorphism?
Deprisoquine
What type of anti-depressants are effected by CYP2D6 metabolism?
Tricyclic ant-depressants
poor metabolizers increase side effects
ultrafast metabolizers degrade drug too quickly
What drug is a proton pump inhibitor and is influenced by CYP2C19 polymorphism?
omeprazole aka Prilosec
What drug is an anti-convulsant and is effected by a CYP2C19 polymorphism?
phenytoin
What drug is an anti-platelet and is effected by a CYP2C19 polymorphism?
clopidogrel
What drug inhibits platelet aggregation and when you not activated due to polymorphism by CYP2C19 leads to decrease in drug activity and increase in serious CV outcoumes?
clopidogrel
What drugs are impacted by CYP2C9 and lead to risk of bleeding/hemorrhage with polymorphisms?
Warfarin
What drug is effected by Vitamin K receptor (VKORC1); and when the clade is different for that VKORC1 leads to different dosing requirements?
CLade A requires low dosing
Clade B requires high dosing
Warfarin
What drug can lead to adverse reactionso f apnea and paralysis when there is a psuedocholinesterase polymorphism?
succinylcholine
What drug increases risk for life threatening bone marrow suppression iin patients with decreased thiopurine methyltransferase activity?
6-mercaptopurine
P-glycoprotein function in the gut results in increase net uptake of what drug?
cardiac glycoside digoxin
What drug is CYP2D6 poor metabolizer and ultrafast metabolizer has what effect on what drug that can increase side effects or have no benefit?
Codeine
ultrafast increases morphine side effects
slow causes codeine no benefit
What drugs metabolism is primarily mediated by CYP2C9, acts as a COX1 and COX2 inhibitor as well as an inhibitor of CYP2D6?
Celecoxib`
What drug helps treat trigeminal neuralgia and is also an anticonvulsant, by acting on Na+ channel to reduce excitability?
carbamazepine
What are the drugs that is a tyrosine kinase inhibitor that target the kinase domain of the EGF receptor and inhibit signaling?
gefitinib
and
erlotinib
What drug is a alpha1, alpha2 and Beta1 agonist Increases Peripheral Vasc Resistance Increase mean BP Therapeutic used for: vasoconstrictor in acute care elevate blood pressure
norepinephrine
What drug is alpha1,alpha2, beta1, beta2 agonist cardiovasc effects: increase HR, contractile force, CO Increase systolic BP, decrease diastolic BP dose-dependent PVR decrease bronchodilation hyperglycemia Used to treat hypersensitivity rxns increase duration of local anesthetics bradyarrhythmias decrease opthalmic hemorrhage
Epinephrine
What drug is a Beta1 and Beta2 agonist
catecholamine
decreases PVR
Increase HR, Contractile force, mean BP decrease
bronchodilation
Emergency Tx of bradycardia or heart block
Isoproterenol
CardioVasc actions of this drug are dose-dependent
low dose: “renal dose” (D1 agonist) increase renal blood flow
intermediate dose “cardiac dose” increase HR, contactile force, cardiac output (Beta1, D1 agonist)
High dose “pressor dose” vasoconstriction and increased peripheral vasc resistance (D1, alpha1, beta1 agonist)
Dopamine
What drug acts overall as a racemic mixture funtions as a Beta1 agonist?
Increase HR, contractility and CO
Short-term Tx of cardiac decompensation
Cardiac stress test
Dobutamine
What is the orally active pro-drug metabolized in nerve terminas and acts as an alpha2 receptor agonist and stimulates central alpha2 to reduce sympathetic outflow.
Major therapeutic use is hypertension
side effects: sedation, dry mouth, edema, rebound hypertension
Methyldopa
What is an agonist of alpha1 adrenergic receptor increase systolic and diastolic blood pressure reflex decrease in heart rate decrease blood flow in most vasc beds Therapeutic use: opthalmic decrease hemorrhage nasal decongestant admin with local anesthetic treatment of hypotestant
Phenylephrine
What is an alpha2 adrenergic receptor agonist
orally active
used as an anti-hypertensive by actions in CNS alpha 2 receptors
causes prolonged blood pressure lowering
decreases PVR, HR, CO
side effects:
dry mouth and sedation, edema, rebound hypertenstion
Clonidine
What is a selective beta2 adrenergic receptor agonist short acting -3-6 hours bronchodilator main therapeutic role adverse effects tremor , anxiety , tachycardia
Albuterol
What is a beta 2 agonist used by inhalation with a long duration of action 12hrs
lipophilic
used to treat COPD, nocturnal or persistant asthma
slow onset of action, not for acute bronchospasm
Salmeterol
What drug is a powerful CNS stimulant in addition to peripheral alpha and Beta receptor actions
depresses appetite
effective after oral admin
molecular actions work by releasing NE from adrenergic nerves, weak direct alpha and Beta agonist, competes with NET
used to treat narcolepsy and ADD
amphetamine
Direct agonist alpha and Beta receptors
orally active
CNS stim
banned by fda
Ephedrine
Direct alpha1, little Beta 2 agonist
less CNS stim
major therapeutic use
decongestant
psuedoephedrine
Inhibits norepi release and depletes neuronal amine stores
orally active, long acting
don’t penetrate into CNS
taken up into adrenergic nerves via NET
Used to treat essential hypertension
side effects:
orthostatic hypotension, male sexual dysfunciton diarrhea
Guanethidine and Guanadrel
What diffuses into adrenergic neurons and depletes norepi stores by inhibitin VMAT2
orally active, penetrates into CNS
used to treat hypertension
Side effect: sedation, depression, diarrehea, gastric issues
reserpine
What drug is an irreversible antagonist of alpha1 and alpha2 recetpors orally active, long duration
produces vasodilation proportional to degree of sympathetic tone
treats hypertension with pheochromocytoma
Phenoxybenzamine
What is a competitive inhibitor of alpha1 and alpha2 receptors
orally active, shorter duration of action 2-4 hours, block can be overcome by increasing level of agonists
hypertension-can only be used in combo with other agents
shorten or reverse DOA of anesthesia
Phentolamine
What drug is an orally active, selective competitive anatagonist of alpha1 receptor
little blockade of presynaptic alpha2
decreases vascular tone
produces favorable effect on lipid profile
treats hypertension, short-term Tx of CHF, first dose phenomenom
Prazosin
What drug is an alpha1A antagonist with less blockade of alpha1B atagonist, treats difficulty urinating associated with benign prostatic hyperplasia
Tamsulosin
What drug is a non-selective Beta antagonist, competitive reversible , has substantial first-pass emtabolism therapeutic for hypertension angina pectoris cardiac arrythmias Acute MI Pheochromocytoma side effect sedation, impotence, increase airway resistance
propranolol
What drug is similar to propranolol, therapeutically, non-selective beta adrenergic receptor antagonist, also treats wide-angle glaucoma admin as eye drops
Timolol
What drug is a 2nd gen beta blocker, Beta1 selective antagonist
competitve, reversible, at low doses is more selective for beta1 receptor
treatment similar to propranolol
treatment of chronic heart failure
less bronchoconstriction
Metroprolol
What drug si a Beta1 selectie antagonist that is orally active, once per day dosing, doesn’t penetrate into CNS, and has similar to propanolol treatment but doesnt do migraine Tx
Atenolol
What 3rd gen beta blocker is a competitive reversiblle antagonist of alpha1 adn both Beta receptors, treats hypertension orally and hypertensive emergencies by IV
Labetolol
What 3rd gen beta blocker is a competitive reversible antagonist of alpha1 and both beta receptors and is sued to treat CHF, hypertension, acute MI
Carvedilol
What muscarinc agonist is used opthalmic for rapid miosis?
acetycholine
What quatenary amine, choline ester, has a primary effect on GI/GU system
Used to treat urinary retention in absence of obstruction
Bethanechol
What alkaloid is a tertiary amine with predominant muscarinic effect, is used orally for xerostomia and amiotic agent to treat wide angle glaucoma and emergency Tx for narrow angle glaucoma?
Pilocarpine
What is the non-substrate, competitve acetylcholinesterase inhibitor
truly reversible
rapid onset short duration
doesn’t penetrate CNS
IV Admin
Used to treat myastehnia gravis
Distinguish cholinergic from myasthenic crisis
reverse paralysis by competitve neuromusc blcking agents
edrophonium
What alkaloid is reversible aceylcholinesterase inhibitor that acts as a slowly reversible substrate
lipophilic, penetrates CNS
treatment of chronic-wide angle glaucoma
treats toxicity by antimuscariic drug poisoning
Physostigmine
What synthetic, slowly reversible, no CNS pen, oral
reversible substrate aceytylcholinesterase inhib is
used for
myasthenia gravis Tx
prevetiono f atony of gut and bladder
reverse of paralysis by neromusc junction blocking
neostigmine
What drugs aare nerve gases, act as irreversible acetylcholinesterase inhibitors?
Sarin, tabun, soman
What is an insectide that can be dangerous as an organophosphate?
parathion
What is an insectide that has greater safety as an organophosphate, becasue it is detoxified in higher organisms?
Malathion
What reactivates Ach peripherally that is used to treat organophosphate toxicity, that must be used quickly in additon to Atropine?
Pralidoxime
What is a muscarinic receptor antagonist that is used to treat organophosphate toxicity?
Previously used for various GI disorder
Tx of :
Bradyarrythmia
mydriasis and cycloplegia
during anesthesia to block vagal reflexes and reduce secretions
Atropine
What muscarinic receptor antagonist is an alkaloid that has great CNS penetrationa
Tx for:
Motion sickness and vestibular disease?
Scopolamine
What semi-synthetic muscarinic receptor antagonist has no CNS penetration and poor systemic absorptionw hen inhaled
reduce bronchial secretions and reduce bronchocontrstion
Tx:
COPD
Ipratropium
What synthetic antagonist of Muscarinic receptor has a fast onset (20-40 min) short duration 4-6 hrs
Tx for:
mydriatic and cycloplegic
Tropicamide
What synthetic muscarinic antagonist is used to Tx: overactive bladder and incontinence
but has high incidence of anti-muscarinic side-effects:
xerostomia, blurred vision, constipation, drowsiness
Oxybutynin
What syntehtic antagonist of muscarinic receptor is used to treat overactive bladder and incontincence and has selectiity for M3 subtype resulting in less CNS side effects?
Darifenacin
What synthetic antagonist of muscarinic receptor is a quaternary amine and has noCNS pen
Tx for:
parasympathomimetic effects when neostigimine is used to reverse skeletal muscle paralysis by neuromusc blocking agent?
glycopyrrolate
What competitive neuromuscular blocking agents has an intermediate duration, with liver metabolism, minimal cardiovasc effects and no histamine release?
Rocuronium
Vecuronium
What competitive neromusc blocking agent has an intermiediate duration, spontaneously degrades in plasma, minimal cardio effects and slight histamine
Atracurium
What competitive neuromuscular blocking agent has a long duration of action, eliminated b renal excretion, causes slight increase in HR and BP and slight histamine release?
Pancuronium
What drug is a depolarizing neuromuscular blocker, that produces muscle fasciculations and paralysis with an ultra-short duration of action
metabolized by pseudocholinesterase and used frequently to allow tracheal intubation?
succinylcholine
What is a competitive antagonist of the leukotriene receptor, used for management and prophylaxis of asthma?
zafirlukast
What inhibits the synthesis of of leukotrienes and is used as prophylaxis and chronic tx of asthma.
zileuton
What drugs act by inhibiting TNF-alpha, acting by binding TNFalpha as a antibody?
Etanercept
infliximab
What drug is an antiplatelet,NSAID and acts by inihibiting COX 1 adn 2 enzymees via acetylation leading to a decrease in prostaglandin precursor formation?
Aspirin
What drug is used for cervical ripening by break down of collagen and EP4 receptor and termination of early pregnancy by EP1/EP3, increase calcium.
Dinoprostone/PGE2
What drug is used to terminate pregnancy by uterine contraction and increase calcium as well as used to tx postpartum hemorrhage after conventional tx?
Carboporst/PGF2alpha
What durg is used as a replacement therapy for prevention of ulcers caused by long-term admin of NSAIDS by suppression of gastric secretiona nd increase mucosal blood flow?
Misoprostol/PGE1
What is used to treat impotence/erectile dysfuction by intracavernous injection as well as maintenance of patent ductus areteriousus until surgical correction?
Alprostadil/PGE1
What is used to tx primary pulmonary hypertension which is rare, done by continuous IV infusion?
Epoprostenol/PGI2
What is used to treat glaucoma by increasing outflow of aqueous humor and EP2/4 receptor as well as used to create eyelash hypotrichosis?
Bimatoprost/PGF2alpha
What drug is an endogenous steroid, frequently used as a tx for adrenal insufficiency?
cortisol
What drug (steroid) has a strong anti-inflammatory potency and causes no sodium retention?
Dexamethasone
What steroid is more similar to cortisol but with a slightly stronger anti-inflammatory property and slightly less mineral corticoid properties?
prednisolone
What steroid tx has both strong anti-inflammatory potency as well as acts strongly as a mineralcorticoid?
Fludocortisone
What endogenous steroid has strong mineralcorticoid properties and minimal anti-inflammatory/glucocorticoid properties?
aldosterone
What drugs blocks 11-beta hydroxylation as a syntehsis inhibitor, doesn’t inhibit ACTH and is used as a diagnostic test/
metyrapone
What durg acts as a competitive antagonist at progesterone and glucocorticoid receptors. Tx Abortiona nd Cushing disease
Mifepristone
What two rugs are competitive at mineralcorticoid receptors. Diureteics that are used to tx hypertensiona nd CHF and hypertrophy?
Sprionolactone and Elperenone
What drug is a progesterone recetpor agonist but a mineralcorticoid antagonist as well as an androgen receptor antagonist. Tx w/ estrogen:: Suppress ovulation and as HRT
Drospirenone
What drug is metabolized to 6-mercaptopurine. Inhibits purine biosynthesis. Tx: Inhibit rejection of transplanted organs and in autoimmune diseases
Azathioprine
What drug is an alkylating agen that resutls in cross-linking of DNA to kill replicating and non-replicating cells. Toxic effect more suppressed on B cells. Used to tx autoimmune diseases.
Cyclophosphamide
What drug is an inhibitor of dihydrofolate reductase, inhibits dna syntehsis and is used to tx autoimmune disease.
Side effect: hepatic diseases
Methotrexate
What durg is metabolized to mycophenolic acid. Mechanism of action: lymphocyte selective immunosuppressant. Cannot make GMP via salvage pathway. Inhibit lmphocyte proliferation and expression of cell surface adhesion molcules. Tx: prevent renal allograft and allows lower dose of cyclosporine. Tx rheumatoid arthritis and refactory psoriasis.
Mycophenolate mofetil
What drug is a lipophilic peptide antibiotic. Mechanism of action is it binds to a cellular receptor to preven actionation of IL2 production. Prevents rejection of transplanted organs and used in some autoimmune diseases.
Nephrotoxicity is a major ide effecct–> reversible
cyclosporine
What drugs is a FK binding protein that has the same mechanism of action as cyclosporine. 50-100x more portent than cyclosporine with less toxicity.
tacrolimus
What durg inhibits t cell activation and proliferation downstream of IL2. Binds FKBP-12. blocks G1 to S transition
Sirolimus
What is the chemical name for aspirin?
Acetylsalicylic acid
What drug has a plasma half life of 2 hours, is an anti-inflammatory, anti-pyretic and analgesic that is a COX1 and COX2 inhibitor. Propionic derivative
Ibuprofen
What drug has anti-inflammatory analgesic and anti-pyretic properties that has a half life of 14 hours. Propionic derived.
Naproxen
What drug is an acetic acid derivative that is a reversible inhibitor of COX 1 and 2. Not routinely used to tx pain and fever.
Indomethacin
What drug is a reverisible inhibitor of COX 1 and 2. Absorbed orally and intramuscularly and highly plasma protein bound. Has some advere effects/toxicity.
Keterolac
What is a reversible inhibitor of COX2 preferably but COX1 stillinhibited. Anti-inflammatory analgesic. Pro-drug , has a long half life
Nabumetone
What drug is a reversible inhibitor of COX1 and 2. Oxicam derivative. Half life 50 hours. Tx: acute and chronic rheumatoid arthritis
Piroxicam
What drug sis a salicylate that functions as an inhibition of IL-1 and TNFalpha, lipoxygenase pathway. No COX inhibition. Used to treat ulcerative colitis, rheumatoid arthritis and AK spondyltiis. Local effect in GI.
Sulfasalazine
What drug is a selective COX2 inhibitor That has a sulfa group. and it used to manage acute pain.
Celecoxib
What drug is a para-aminophenol derivative. Mechanism of action is not well understood but is more CNS selective. Only analgeesic and anti-pyretic effects with no anti-inflammatory effects.
Acetaminophen
What agent inhibits the relase of histamine, is an ant-inflammatory agent. Stabilizes most mast cell membrane and prevents histamine release. Prevents asthma, allergic rhinitis, conjunctivitis and food allergies.
Cromolyn sodium
What drug inhibits the release of histamine as a monoclonal antibodies. Can cause hypersensitivity. Subq admin. decreases amnt of antigen specific IgE that normall binds to and sensitize mast cells. Tx allergic asthma.
Omalizumab
What are teh two first generation. Ethanolamines. Antihistimine, general anti-histamine effects, with CNS effects
Diphenhydramine (profound drowsiness) and Dimenhydrinate
What first generation anti-histamine is an alkylamine? Less prone to cause drowsiness.
Cholorpheniramine
What first generation H1 blockers is also a dopamine2 blcoker. Phenothiazines.
Promethazine
What is a second generation antihistamine that has a higher incidence of sedation than the others? Is derived from piperazines.
cetirizine
What H2 receptor blockers offer relief of symptoms of gastric upset and has a main tx uncomplicated Gastroesophageall reflux? Therefroe have a low incident of side effects. In order of potency from most potent to least.
Famotidine>Ranitidine>Cimetidine
What H2 receptor blockers is inhibits cytochrome P450, long term at high doses decreases testosterone binding.
Cimetidine
What H2 receptor blocker inhibits cytochrome P450 at 10% of the rate of cimitedine?
ranitidine
What are the three second generation of antihistamine drugs.
fexofenadine, loratadine and desloratadine
What is a potent hallucinogen, a full or partial agonist at 5HT2 receptor?
Lysergic Acid Diethylamide
What is a partial agonist at 5HT1A receptors used as an antianxiety agent?
Buspirone
What is an agonist at 5HT1D?
Tx used in migraine headaches
side effects nausea, vomiting, angina, dizziness and flushing
Sumatriptan
What is an indirect agnoist of serotnin. Blocks reuptake of serotonin into neurons.
Tx affective disorders
OCD
Panic attacks
Fluoxetine
What is an indirect agonist of serotonin? Monoamine oxidase inhibitors– block metabolism of serotonin, NE and DA
Tx of depression and narcolepsy. Food induced HTN
Phenelzine
What is a 5HT2 receptor antagonist as well as a H1 histamine antagonist?
Cyproheptadine
Tx of skin allergies, pruritus
carcinoid
What is a 5-HT3 receptor antagonist?
Tx: nausea and vomitting from chemo
GI and brain receptor
Odansetron
What is a selective 5HT3 antagonist used to tx women with predominant IBS
Alosetron
What is a nitrate involved in relaxation of arterial and venous smooth muscle.
Heart failure
toxicity-hypotension.
Mechanism of action of nitrates is NO donor, intracellular signaling
(venous dominant)
nitroglycerin
What drug is involved in relaxation of arterial and venous circulations.
Heart failure
Hypotension
Nitroprusside
What direct vasodilator, inolved in arterial circulation. Heart failure, hypotension?
Mechanism of action: increases cGMP
Tx hypertension emergencies
hydralazine
direct vasodilator; Tx severe hypertension K+ATP channel opener Arterial circulation Fluid retention-use with diuretics
minoxidil
What potassium channel opener is used to treat hypertensive emergencies and hypoglycemia
Diazoxide
What calcium channel blocker is pheylalkylamine?
verapamil
What calcium channel blocker is benzothiazapine?
diltiazem
What are the phosphodiesterase 3 inhibitors. Tx Heart failure through intracellular signaling
Milrinone, Inamrinone, Cilostazol
What are the phosphodiesterase 5 inhibitors, used to tx erectile dysfunction?
Sidenafil, Tadalafil
What drug is involved in renin-angiotensin blocker. Treats by renin inhibition, lowering arterial and venous circulation?
Angiotensin converting enzyme inhibitor
What drug is a vasodilator, works by dopamine A1 receptor agonists Arteriial and venous circulation.
Involved in renal blood flow and Na secretion
Tx hypertensive crisis
Fenoldopam
What drug is an alpha-adrenergic blocker. Involved and venous circulation
Prazosin
What bronchodilators are Beta2 agonists?
albuterol, pirbuterol, Terbutaline, salmeterol, formoterol
have some cardiotoxicity
What drug is an anti-cholinergic, works by muscarinic receptor and mucous secretion.
Ipratropium, Tiotropium
What drug is a bronchodilator, using methylxanthine. Phosphodiesterase inhibition. Adenosinereceptor antagonism
Theophylline, aminophylline