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0107 - Pharm Flashcards

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1
Q

What is half-life given Vd and clearance?

A

t1/2 = (Vd x 0.7) / clearance

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2
Q

Efficacy vs. potency

A

Efficacy = intrinsic ability of drug to elicit an effect (maximum effect). E.g. analgesics, abc, antihistamines, decongestants. Potency = dose of drug required to produce a given affect (Km related). Highly potent drugs include chemo, antiHTN, lipid-lowering. Potent dose, Kim! Max, more efficacious please.

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3
Q

Vd = ?

A

= amount of drug given (mg) / plasma concentration of drug (mg/L) = theoretical volume occupied by total absorbed drug amount at plasma concentration.

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4
Q

CYP 450 Inducers

A

Chronic alcohol, Modafinil, St. John’s wort, Phenytoin, Phenobarbital, Nevirapine, Rifampin, Griseofulvin, Carbamazepine. “Grisly St. John Nevir Riffs the Phen-Phen w/o Carbs, Chronic Alcohol, or Modafinil.”

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5
Q

CYP 450 inhibitors

A

Acute alcohol, Gemfibrozil, Ciprofloxacin, INH, grapefruit, quinidine, amiodarone, ketoconazole, macrolides, sulfonamides, cimetidine, ritonavir. “‘Cip A-Cute Macro Grapefruit at the NIH,’ (w)Rit an Amiable Keto Quinn w/ a Sulfur-colored Gem’d Cimetar.”

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6
Q

Two major variables in M-M kinetics?

A

Km = 1 / affinity. Vmax is proportional to enzyme concentration. At Km concentration, 1/2 Vmax velocity.

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7
Q

Lineweaver-Burk

A

y-intercept = 1/Vmax. X-intercept = -1/Km (Closer to 0, greater the Km, weaker affinity)

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8
Q

Competitive vs. non-competitive inhibitors on Lineweaver-Burk

A

Competitive inhibitors do NOT affect Vmax = same y-intercept. Non-comp inhibitors do NOT affect affinity -> same x-intercept

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9
Q

Reversible, non-reversible comp inhibitors, and non-comp inhibitors potency vs. efficacy?

A

Reversible comp - don’t change Vmax but change Km. decreased potency. Non-reversible competitive and non-competitive inhibitors change Vmax -> decrease efficacy.

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10
Q

Pharmacokinetics vs. Pharmacodynamics

A

Kinetics are body’s effect on drug. ADME = absorption, distribution, metabolism, excretion. Dynamics is affect of drug on body - receptor binding, efficacy, potency, toxicity.

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11
Q

Bioavailability

A

Fraction (F) of drug that reaches systemic circulation unchanged. IV is 100%.

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12
Q

Low, Middle, High Vd tells you what?

A

Vd is LOW (4-8L) if drug remains in plasma (bound to plasma proteins, hydrophilic b/c charged). High Vd (e.g. 41) are small MW AND uncharged; in all tissues + fat. Medium Vd (teens) for small MW and hydrophilic b/c in interstitium (ECF).

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13
Q

What do I need to know about half-life?

A

t1/2 = 0.7 x Vd / clearance. Drug infused at constant rate takes 4-5 half-lives to reach SS. (3.3 half-lives to reach 90% of SS). 1:50% remaining, 2:25%, 3:12.5%, etc.

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14
Q

Clearance

A

Volume of plasma cleared of drug per unit time = rate of elimination of drug / plasma concentration = Vd x Ke (elimination constant)

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15
Q

Loading dose calculation

A

Cp x Vd / F where Cp = target plasma concentration at SS.

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16
Q

Maintenance dose calculation

A

Cp x CL x tau / F where tau = dosage interval.

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17
Q

Zero-order elimination vs. 1st-order elimination

A

Constant rate of elimination (e.g. PEA - Phenytoin, Ethanol, Aspirin) vs. constant fraction is eliminated

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18
Q

Trapping drugs in urine?

A

Ionized forms are trapped and cleared quickly. Weakly acidic drugs (e.g. phenobarbital, MTX, ASA) can be cleared with bicarbonate. Weakly basic drugs (e.g. amphetamines) can be cleared with ammonium chloride.

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19
Q

Phase I vs. phase II drug metabolism.

A

I - CYP450 reduction, oxidation, and hydrolysis leading to slightly polar, water-soluble metabolites. II - GAS (Glucorinidation, Acetylation, and Sulfation) leading to VERY polar, inactive metabolites.

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20
Q

Therapeutic index

A

TITE = TD50/ED50 = median toxic dose / median effective dose. Higher therapeutic index is a SAFER drug.

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21
Q

Sympathetic vs. parasympathetic pathway for cardiac and smooth muscle, gland cells, and nerve terminals

A

Sympathetic - pre-ganglion to chain (ACh). Post-ganglion to muscle (NE, alpha and beta adrenergic receptors). Parasympathetic - pre-ganglionic from medulla. Synapse (ACh), then post-ganglion to muscle (ACh, M receptor)

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22
Q

Sympathetic sweat glands pathway?

A

Chain w/ ACh. Post-ganglionic w/ ACh, M.

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23
Q

Sympathetic renal vasculature pathway?

A

Chain w/ ACh. Post-ganglionic with D, D1. Kidneys are dope, sweat is musty, and the rest is adrenergic.

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24
Q

Adrenal medulla pathway?

A

Directly ACh -> Epi and NE release

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25
Nictonic vs. Muscarinic receptors?
Both are ACh receptors. N are ligand-gated Na+/K+ channels. Nn in autonomic ganglia. Nm in NMJ. Muscarinic receptors are GPCRs that act thru 2nd messengers. M1-5.
26
Dopamine GPCRs?
D1 - Gs, relaxes renal vascular SMC. D2 - Gi, modulates transmitter release (esp. brain). Kidneys are DOPE. Brain is okay.
27
Histamine GPCRs
H1 - Gq, increase mucus production, vascular permeability,, contraction of bronchioles, pruritus and pain. H2 - Gs, increased gastric acid secretion. H1 is allergies. H2 is ranitidine.
28
Vasopressin GPCRs
V1 - Gq, increased vascular SMC contraction. V2 - Gs, increased water permeability and reabsorption in collecting tubules of kidney.
29
Parasympathetic GPCRs
M1 - Gq, CNS and enteric (brain is first). M2 - Gi, decreased HR and contractility of atria (heart is second). M3 - Gq, inc. exocrine gland secretion, inc. peristalsis, inc. bladder contraction, bronchoconstriction, miosis, accomodation
30
Sympathetic GPCRs
a1- Gq, vasc SMC contraction, mydriasis, increased intestinal and bladder sphincter contraction. a2 - Gi, decreased sympathetic outflow, decreased insulin, dec lipolysis, inc. PLT aggregation. B1 - Gs, inc HR, inc contractility, inc renin, inc lipolysis. B2 - Gs, vasodilation, bronchodilation, inc HR, inc contractility, inc lipolysis, inc insulin, tocolysis, ciliary muscle relaxation (un-accmodate), inc. aqueous humor
31
Acronym for GPCR systems
Sympathetics, Parasympathetics (M1-M3), Dopamine, Histamine, Vasopress. Qiss and Qiq till your siq of sqs
32
Amphetamines
Activates NE release and inhibits reuptake. For narco, obesity, ADHD
33
NE reuptake inhibitors
Amphetamines, cocaine, TCAs
34
Modulation of NE release?
NE negatively feedbacks via alpha-2 receptors. Angiotensi-II activates NE release.
35
Where do ACh esterase inhibitors act?
Post-synaptic membrane
36
Gq GPCR receptors?
HAVe 1 M&M - H1, alpha1, V1, M1, M3
37
Gi GPCR receptors?
MAD 2's - M2, alpha2, D2
38
Cholinomimetic agents
Bethanechol, carbachol, pilocarpine, methacholine.
39
Bethanechol
Postop ileus, neurogenic ileus, urinary retention. Activates Bowel and Bladder SMC. Resistant to AChe. Bethany, let it go!
40
Carbachol
Glaucoma, pupillary constriction, intraocular pressure.
41
Pilocarpine
Stimulator of sweat, tears, saliva. Open (contracts ciliary muscle) and closed-angle glaucoma (constricts pupillary sphincter).
42
Methacholine
Asthma challenge.
43
Indirect agonists for ACh
Neostigmine, Pyridostigmine, Physostigmine, Donepezil/rivastigmine/galatamine, Edrophonium
44
Neostigmine
Post-op and neurogenic ileum, urinary retention, myasthenia gravis, reverse NMJ blockade. Neo = NO CNS penetration.
45
Pyridostigmine
Long-acting for Myasthenia. No CNS
46
Physostigmine
ACh toxicity (Crosses CNS)
47
Cholinesterase inhibitor poisoning
DUMBBELSS - Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of m. and CNS, Lacrimation, Sweating, Salivation. Tx = atropine (Ach antagonist) + pralidoxime (AChE regenerator)
48
GU Muscarinic antagonists
Reduce urgency in mild cystitis and bladder spasms. Oxybuynin, darifenacin, solifenacin
49
Respiratory muscarinic antagonists
Ipratropium, tiotropium - COPD, asthma
50
CNS muscarininc antagonists
Benztropine for Parkinsons. Scopolamine for motion sickness.
51
GI, resp muscarininc antagonist
Glycopyrrolate - reduce airway secretions, drooling tx, peptic ulcer tx
52
Atropine effects
Pupil dilation, cycloplegia, dec. airway secretions, dec. acid secretions, decreased motility, decreased urgency in cystitis.
53
Atropine toxicity
Hot as hare, Dry as bone, Red as beet Blind as a bat (cycoplegia), Mad as a hatter.
54
Epinephrine
B > alpha. Inds - anaphylaxis, OA-glaucoma, asthma, hypotension
55
Norepinephrine
alpha1>alpha2>beta. Use for hypotension (but decreased renal perfusion)
56
Isoproterenol
B1=B2. Beta2-mediated vasodilation -> dec. pressure -> increased HR. Inds - for evaluating tachyarrhythmias.
57
Dopamine
D1 = D2 > Beta > alpha. Ind for unstable bradycardia, HF, shock. Inotropic and chronotropic alpha effects at high doses
58
Dobutamine
Beta1 > Beta2, alpha. HF, cardiac stress testing
59
Phenylephrine
alpha1 > alpha2. Hypotension, mydriasis, rhinitis (Decongestant)
60
Albuterol, salmeterol, terbutaline
B2 > B1. Acute asthma, COPD. Terbutaline for tocolysis in premature contractions.
61
Ephedrine
Nasal decongestion, urinary incontinence, hypotension
62
Sympatholytics
alpha-agonists. Clonidine and alpha-methyldopa.
63
Clonidine
Clonidine is used for HTN urgency, ADHD, severe pain. Toxicities include CNS depression, brady, hypo, resp depression, miosis.
64
alpha-methyldopa
Used for HTN in pregnancy. Tox -> Direct Coombs + hemolytic anemia.
65
Non-selective alpha blockers
Phenoxybenzamine and phentolamine
66
Phentolamine
Reversible. Used to reverse hypertensive crisis in MAOi taking patients who ate tyramine.
67
Phenoxybenzamine
Irreversible. Used for pehochromocytoma pre-op to prevent HTN crisis
68
Alpha-1 antagonist
=-osins (Prazosin, terazosin, tamsulosin). Used for BPH urinary symptoms, HTN. Tox - 1st dose hypotension.
69
Alpha-2 antagonist
Mirtazapine used for depression. Tox = sedation, inc. chol, inc appetite
70
B1>B2 selective antagonists
A to M. Atenolol, esmolol, metoprolol
71
Non-selective Beta blockers
N to Z. Nadolol, propanolol, timolol
72
Nonselective alpha AND beta-antagonists
Carvedilol and labetalol
73
Beta blocker toxicities
Impotence, CNS, CV, dyslipidemia (metoprolol), exacerbate asthmatics and COPD, cocaine risk-> HTN
74
Beta-blocker tox tx?
Glucagon
75
Cu, As, Au fox treatment?
Penicillamine
76
Cyanide treatment?
Nitrite + thiosulfate, hydroxocobalamin
77
Digitalis fox treatment?
Anti-digitalis Fab fragments
78
Fe tox treatment?
Deferoxamine, deferasirox
79
Lead tox treatment?
EDTA, dimeraprol, succimer, penicillamine
80
Mercury, arsenic, gold tox treatment?
Dimercaprol, succimer
81
Methanol, ethylene glycol tox treatment?
Fomepizole > ethanol, dialysis
82
Methemoglobin tox treatment?
Methylene blue, Vitamin C
83
Salicylate tox treatment?
NaHCO3, dilaysis
84
TCAs tox treatment?
NaHCO3 (plasma alkalinization)
85
tPA, streptokinase, urokinase tox treatment?
Aminocaproic acid
86
Coronary vasospasm drugs?
Cocaine, sumatriptan, ergot alkaloids
87
Cutaneous flushing drugs?
VANC - vanc, adenosine, niacin, Ca2+ channel blockers
88
Dilated cardiomyopathy drugs?
Doxorubicin, daunorubicin
89
Torsades de pointes causing drugs?
Class II, IA, macrolides, antipsychs, TCAs
90
Hyperglycemia causing drugs?
Tacrolimus, PIs, Niacin, HCTZ, Beta-blockers, Corticosteroids
91
Hypothyroidism causing drugs?
Li, amiodarone, sulfonamides
92
Focal to massive hepatic necrosis drugs?
HAVAc - halothane, Amanita phalloides, Valproic acid, acetaminophen
93
Pancreatitis causing drugs?
Didanosine, Corticosteroids, Alcohol, Valproic, Azathioprine, Diuretics. "Drugs Causing Violent Abdominal Distress."
94
Agranulocytosis causing drugs?
Dapsone, Clozapine, Carbamazepine, Colchicine, Methimazole, Propylthuiouracil
95
Aplastic anemia causing drugs?
Carbamazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, Propylthiouracil. "Can't Make New Blood Cells Propylerly."
96
Hemolysis in G6PD?
INH, Sulfa, Dapsone, Primaquine, ASA, Ibuprofen, Nitrofurantoin. "Hemolysis IS D PAIN"
97
Megaloblastic anemia causing drugs?
Phenytoin, Methotrexate, Sulfa. "Having a blast with PMS?"
98
Fat redistribution drugs
PIs, Glucocorticoids
99
Gout causing drugs?
Pyrazinamide, thiazides, furosemide, niacin, cyclosporine "Painful Tophi on Feet Need Care" in gout.
100
Photosensitivity drugs?
Sulfonamides, Amiodarone, Tetracyclines, 5-FU. "SAT For a photo."
101
Stevens-Jonson drugs
Anti-epileptics, allopurinol, sulfa, penicillin
102
SLE like syndrome drugs?
Sulfa, hydralazine, INH, procainamide, phenytoin, etanercept. "Lupus is SHIPP-E"
103
Drugs causing seizures?
INH, bupropion, Imipenem/cilastatin, tramadol, enflurane, metoclopramide. With seizures, I BITE My tongue
104
Drugs causing SIADH?
Carbamazepine, cyclophosphamide, SSRIs
105
Drugs causing pulmonary fibrosis?
Bleomycin, amiodarone, busulfan, methotrexate
106
Substrates for P450?
Always Always Always Always Think When Starting Others. (Anti-eps, antideps, anti-psychs, anesthetics, theophylline, warfarin, statins, OCPs).
107
Sulfa drugs
Popular FACTSSS - Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine, Sulfonylureas.
108
-Azole vs. -bendazole?
Ergosterol synthesis inhibitor vs. Antiparasitic/helmintic
109
Digoxin mechanism
Inhibits Na-K-ATPase increasing intracellular Na+, decreasing trasmembrane sodium gradient that drives Na-Ca transporter -> ca+ accumulation in the cell. Larger amount of Ca+ from SR released -> more cross-bridges. Inotrope but AV nodal blockage (increased diastolic filling time).

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