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94 Cards in this Set
- Front
- Back
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Vmax is dependant on...
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enzyme concentration
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increase Km = _ affinity
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decreased
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volume of distribution
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relates the amount of drug in the body to amount of drug in plasma.
amt of drug in body/plasma drug [ ] |
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Low Vd
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distributes in blood
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high Vd
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distribute in all tissues
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clearance
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UxV / Px
Ux = urine concentration of drug x V = urine flow rate (usu 1mL/min) Px = plasma concentration of drug x |
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A drug infused at a constant rate takes how many half-lives to reach steady state?
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4-5
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Zero order elimination
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rate of elimination is constant regardless of plasma concentration
constant AMOUNT of drug is eliminated per unit time |
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Zero-order drug examples
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Phenytoin
Ethanol Aspirinl (a PEA is round, like the # zero) |
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First order elimination
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Constant fraction of drug is eliminated per unit time.
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OD on aspirin, phenobarbital or methotrexate. How would you alter urine pH to help?
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These are weak acids that are trapped in alkaline environment
Alkalinize urine with bicarbonate, silly! |
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OD on amphetamines, how would you alter the urine to help?
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amphatamines = weak base
Acidify the urine with ammonium chloride. |
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Efficacy defined:
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maximal effect a drug can produce
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Potency
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amount of drug needed for a given effect
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Competitive antagonist
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shifts dose response curve to the RIGHT (dec potency, no change on efficacy)
ex: diazepam and flumazinil on GABA-receptor |
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Noncompetitive antagonist
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Shifts dose response curve LEFT (dec efficacy)
ex: NE and phenoxybenzamine on alpha-R |
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Partial agonist
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Reduced maximal effect (dec efficacy).
ex: morphine and buprenorphine at opioid mu receptor |
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Therapeutic index
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TI = LD50 / ED50
TILE |
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Direct cholinomemetic drugs (4)
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1. Bethanechol
2. Carbachol 3. Pilocarpine 4. Methacholine |
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Bethanechol
uses and MOA |
MOA: activates bowel and
uses: bladderilieus and urinary retention |
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Carcachol
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MOA: CARBon copy of ACh
uses: glaucoma, pupillary contraction and relief of IOP. |
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Pilocarpine
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MOA: contracts ciliary muscle of eye (open angle) and pupillary sphincter (narrow angle)
uses: potent stim of sweat, tears and saliva |
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Methacholine
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Challenge test for asthma
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Indirect cholinomemetics
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1. Neostigmine
2. Pyridostigmine 3. Edrophonium 4. Physostigmine 5. Echothiophate |
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Neostigmine
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uses: ileus, urinary retention, MG, reversal of neuromuscular blockade
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Pyridostigmine
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uses: MG
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Edrophonium
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uses: Diagnosis of MG
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MOA of all Indirect cholinomimetics
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Inc endogenous ACh
Physostigmine is the only one that crosses the BBB |
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Physostigmine
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Glaucoma and atropine OD
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Muscarinic blockers
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1. Atropine
2. Benztropine 3. Scopolamine 4. Ipratropium |
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Atropine
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In the eye, produces mydriasis and cycloplegia
Blocks DUMBBEELS Can cause acute narrow angle glaucoma in the elderly, urinary retention in BPH |
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Benztropine
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Parkinson's disease
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Scopolamine
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Motion sickness
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EPI
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Direct acting sympathomimetics
uses: anaphylaxis, open-angle glaucoma, asthma, hypotension |
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NE
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Direct acting sympathomimetics
uses: hypotension (dec renal perfusion) |
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Dopamine
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D1 = D2 > beta > alpha
inotropic and chronotropic uses: shock (inc renal perfusion), heart failure |
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Dobutamine
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B1>B2
inotropic (not chronotropic) uses: heart failure, cardiac stress test |
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Phenylephrine
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Direct acting sympathomimetics
a1> a2 pupillary dilation, vasoC, nasal decongestion |
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Albuterol
(also metaproterenol, terbutaline, salmeterol) |
selective B2 agonists
Metaproterenol and Albuterol = acute asthma Salmeterol = long term asthma txmnt Terbutaline = reduce premature uterine contractions |
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Amphetamine
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Indirect sympathomimetics
MOA: releases stored catecholamines uses: narcolepsy, ADD |
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Ephedrine
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Indirect sympathomimetics
MOA: releases stored catecholamines uses: nasal decongestant, urinary incontinence, hypotension |
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Cocaine
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Indirect sympathomimetics
MOA: uptake inhibitor uses: vasoC and local anesthesia |
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Clonidine, alpha-methylDOPA
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MOA: centrally acting alpha-2 agonists, decrease central adrenergic outflow
Uses: HTN, esp with renal disease or pregnancy |
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Phenoxybenzamine (irreversable) and phentolamine (reversible)
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MOA: nonselective alpha blockers
Uses: pheochromocytoma toxicity: orthostatic hypotension, reflex tachy |
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"--zosin" drugs
(Prazosin, terazosin, doxazosin) |
Alpha 1 selective blockers
uses: HTN, urinary retention in BPH toxicity: 1st dose O.hypotension, dizziness, HA |
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Mirtazepine
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Alpha 2 selective blocker
uses: depression toxicity: sedation, inc appetite, hypercholesterol |
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Beta blocker toxicity
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Impotence
Asthma exacerbation CV = (brady, AV block, CHF) CNS = (sedation, sleep alteration) Use with caution in diabetics |
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How do beta blockers tx HTN?
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dec cardiac output
dec renin secretion (due to beta-blockade on JGA cells) |
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How do beta blockers tx angina pectoris?
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dec HR and contractility reducing the O2 consumption of heart
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How do beta blockers tx MI?
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dec mortality
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How do beta blockers tx SVT?
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dec AV conduction velocity (class II)
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How do beta blockers tx glaucoma (timolol)
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dec secretion of aqueous humor.
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Acetaminophen antidote/tx
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N-acetylcysteine
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ASA antidote/tx
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NaHCO3 (alkalinize urine)
Dialysis |
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Amphetamine antidote/tx
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acidify urine with NH4Cl (ammonium chloride)
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AChE Inhibitors, organophosphate antidote/tx
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Atropine
2-PAM (pralidoxime) |
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Antimuscarinic agents
Anticholinergic agents antidote/tx |
Physostigmine salicylate
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Beta blockers antidote/tx
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glucagon
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Iron
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Deferoxamine
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Methemoglobin
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Methylene blue, vitamin C
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Carbon monoxide
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100% O2, hyperbaric chamber
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Methanol, ethylene glycol
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Ethanol
Dialysis Fomepizole |
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Opiods
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Naloxone
Naltrexone |
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Benzos
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Flumazenil
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TCAs
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NaHCO3 (plasma alkalinization)
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Heparin
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Protamine
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Warfarin
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vit K
FFP |
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tPA, streptokinase
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Aminocaproic acid
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Theophylline
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beta blocker
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MOA of fomepizil
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inhibits alcohol dehydrogenase
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What drug/class:
atropine-like side effects |
TCAs
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coronary vasospasm
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cocaine
sumatriptan |
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Cutaneous flushing
(VANC) |
Vancomycin
Adenosine Niacin CCB |
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Dilated cardiomyopathy
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Doxorubicin (chemo)
Daunorubicin |
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Agranulocytosis
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Clozapine
Carbamazepine Colchicine Propylthiouracil Methimazole Dapsone |
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Gray baby syndrome
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Chloramphenicol
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Pseudomembranous colitis
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Clindamycin
Ampicillin |
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Gynecomastia
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Spironolactone
Digitalis Cimetidine chronic Alcohol use Estrogens Ketoconazole |
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Hypothyroid
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Lithium
Amiodarone |
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Gingival hyperplasia
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Phenytoin
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Gout
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Furosemide
Thiazides |
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Osteoporosis
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Corticosteroids
Heparin |
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Photosensitivity
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Sulfonamides
Amiodarone Tetracyclines |
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Steven Johnsons
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Ethosuximide
lamotrigine carbamazepine phenobarbitol phenytoin sulfa drugs penicillin allopurinol |
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SLE-like syndrome
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Hydralazine
INH Procainamide Phenytoin |
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Tendonitis, tendon rupture and cartilage damage (kids)
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Fluoroquinolones
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Cinchonism
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Quinidine
Quinine |
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Extrapyramidal effects
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Haloperidol
Chlorpromazine Reserpine Metoclopromide |
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Diabetes Insipedus
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Lithium
Demeclocycline |
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Disulfram like reactions
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Metronidazole
some cephalosporins (3rd gen) procarbazine 1st gen sulfonylureas |
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p450 inducers
Queen barb steals phen-phen and chronically refuses greasy carbs |
Quinidine
Barbs St. John's wort Phenytoin chronic EtOH use Rifampin Griseofulvin Carbemazepine |
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p450 inhibitors
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HIV protease inhibitors
Ketoconazole Erythromycin Grapefruit juice Acute EtOH use Sulfas INH Cimetidine |
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Disulfram MOA
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Inhibits acetaldehyde dehydrogenase
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Sulfa drugs
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Celecoxib, furosemide, probenecid, thiazides, TMP-SMX, acetazolamide and anything with "sulfa" in it.
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