First Aid Pharmacology

Front 1

Michaelis-Menton kinetics

Back 1

Km - inversely related to affinity of enzyme for substrate

Vmax - directly proportional to enzyme concentration

Front 2

Lineweaver-Burk plot

Back 2

Inc. y-intercept, dec. Vmax

Inc. x-intercept (toward O), inc. Km

Front 3

Competitive inhibitors, reversible

Resemble substrate:

Overcome by inc. [S]:

Bind active site:

Effect on Vmax:

Effect on Km:

Pharmacodynamics:

Back 3

Competitive inhibitors, reversible

Resemble substrate: Yes

Overcome by inc. [S]: Yes

Bind active site: Yes

Effect on Vmax: Unchanged

Effect on Km: Increase

Pharmacodynamics: decrease potency

Front 4

Competitive inhibitors, irreversible

Resemble substrate:

Overcome by inc. [S]:

Bind active site:

Effect on Vmax:

Effect on Km:

Pharmacodynamics:

Back 4

Competitive inhibitors, irreversible

Resemble substrate: Yes

Overcome by inc. [S]: No

Bind active site: Yes

Effect on Vmax: Decrease

Effect on Km: Unchanged

Pharmacodynamics: Decrease efficacy

Front 5

Noncompetitive inhibitors

Resemble substrate:

Overcome by inc. [S]:

Bind active site:

Effect on Vmax:

Effect on Km:

Pharmacodynamics:

Back 5

Noncompetitive inhibitors

Resemble substrate: No

Overcome by inc. [S]: No

Bind active site: No

Effect on Vmax: Decrease

Effect on Km: Unchanged

Pharmacodynamics: Decrease efficacy

Front 6

Enzyme inhibition graph

Back 6

Front 7

Bioavaliability

Back 7

Fraction of drug reaching systemic circulation unchanged (F)

Front 8

Bioavalibility: IV and Oral

Back 8

IV: F = 100%

Oral: F <100% - incomplete absorption and first-pass metabolism

Front 9

Volume of distribution (Vd)

Back 9

Volume occupied by total amount of drug in body relative to its plasma concentration

Front 10

Low Vd

Compartment:

Drug types:

Back 10

Compartment: Blood

Drug types: Large/charged molecules; plasma protein bound

Apparent Vd of plasma protein-bound drugs can be altered by liver/kidney disease (dec. protein binding, inc. Vd)

Front 11

Medium Vd

Compartment:

Drug types:

Back 11

Medium Vd

Compartment: ECF

Drug types: small hydrophilic molecules

Front 12

High Vd

Compartment:

Drug types:

Back 12

High Vd

Compartment: All tissues including fat

Drug types: Small lipophilic molecules, especially if bound to tissue protein

Front 13

Clearance (CL)

Back 13

CL = Vd x Ke (elimination constant)

Decreased with cardiac, hepatic, renal problems

Front 14

Half-life

Back 14

Property of first-order elimination

Front 15

More half-life info:

How many half-lives until drug infused at constant rate reaches steady-state?

How many half-lives until it reaches 90% of steady-state level?

Half-life chart: # half-lives and % remaining

Back 15

Infused drug at constant rate takes 4-5 half-lives to reach steady state

Takes 3.3 half-lives to reach 90% of steady state level

Front 16

Loading dose

Back 16

Cp = target plasma [ ] at steady state

Vd = distribution volume

F = bioavailability

Unchanged by liver/renal disease

Front 17

Maintenance dose

Back 17

Cp = target plasma [ ] at steady state

Tau = dosage interval (if not given continuously)

F = bioavailability

Decreased by liver/renal disease

Front 18

Zero-order elimination

Back 18

Constant rate of elimination, regardless of Cp

- Constant amount eliminated with time

- Cp decreases linearly with time

- Capacity-limited elimination

Phenytoin, Ethanol, and Aspirin - PEA is shaped like 0

Front 19

First-order elimination

Back 19

Elimination rate directly proportional to [drug]

- Constant fraction eliminated with time

- Cp decreases exponentially with time

- Flow dependent elimination

Front 20

Trapped in urine/cleared in urine or reabsorbed?

Ionized species:

Neutral species:

Back 20

Trapped in urine/cleared in urine or reabsorbed?

Ionized species: Trapped/cleared

Neutral species: Reabsorbed

Front 21

Urine pH and drug elimination

Weak acids

Back 21

Weak acids

- Trapped in basic environments

- Treat overdose with bicarbonate

RCOOH <=> RCOO- + H+

(Lipid soluble) (Trapped)

Ex: phenobarbital, methotrexate, aspirin, TCAs

Front 22

Urine pH and drug elimination

Weak bases

Back 22

Weak bases

- Trapped in acidic environments

- Treat overdose with ammonium chloride

RNH3+ <=> RNH2 + H+

(Trapped) (Lipid soluble)

Front 23

Drug metabolism: Phase I

Back 23

Reduction, oxidation, and hydrolysis with cytochrome P-450

Yields slightly polar, water-soluble metabolites

- May still be active

Lost by geriatrics first

Front 24

Drug metabolism: Phase II

Back 24

Conjugation (Glucuronidation, Acetylation, Sulfation)

Yields polar, inactive metabolites - renally secreted

Geriatric patients have GAS

Slow acetylators: dec. metabolism, inc. side effects

Front 25

Efficacy

Back 25

Max effect drug can produce

- Y-value = Vmax

- Inc y = inc Vmax = inc efficacy

- Unrelated to potency

Front 26

Potency

Back 26

Amount of drug needed for a given effect

- Inc potency (dec EC50) = less drug needed

- X-value = EC50

- Left shift = dec EC50 = inc potency

- Unrelated to efficacy

Front 27

Competitive agonist

Shift curve?

Effect on potency or efficacy?

Overcome by increasing [S]?

Example

Back 27

Competitive agonist

Shift curve right

Dec potency

Overcome by inc [S]

Flumazenil vs. diazapam (agonist) on GABA receptor

Front 28

Noncompetitive agonist

Shift curve?

Effect on potency or efficacy?

Overcome by increasing [S]?

Example

Back 28

Noncompetive agonist

Shift curve down

Dec efficacy

Not overcome by inc [S]

Phenoxybenzamine vs. norepinephine (agonist) on alpha-receptors

Front 29

Partial agonist

Shift curve?

Effect on potency or efficacy?

Overcome by increasing [S]?

Examples

Back 29

Acts on same site as full agonist but with lower max effect (dec efficacy)

- Potency is an independent variable

Buprenorphine vs. morphine (full agonist) at opioid mu-receptors

Front 30

Therapeutic index

Back 30

TD50/ED50 = median toxic dose/median effective dose

Safe drugs: high TI

Low TI: Digoxin, lithium, theophylline, warfarin

LD50 (lethal) often replaces TD50 in animal studies

Front 31

Back 31

Adrenal medulla and sweat glands are part of sympathetic nervous system but are innervated by cholinergic fibers

Botulinum toxin prevents release of ACh at cholinergic terminals

Front 32

ACh receptors

Nicotinic

Muscarinic

Back 32

NAChR: ligand-gated Na+/K+ channels

- Nn (autonomic ganglia) and Nm (neuromuscular junction)

MAChR: G-protein-coupled recptors

- Act through second messengers

- 5 subtypes: M1through M5

Front 33

G-protein-linked 2nd messenger mnemonic

Back 33

Qiss and qiq until you're siq of sqs

alpha (1, 2) beta (1, 2) m (1,2,3) d (1,2) h (1,2) v (1,2)

Front 34

Alpha receptors

Back 34

Sympathetic

Alpha 1 - q

Inc: vascular smooth muscle contraction, pupillary dilator muscle contraction (mydriasis), intestinal and bladder sphincter contraction

Alpha 2 - i

Dec: sympathetic outflow, insulin release, lipolysis, aqueous humor production

Inc: platelet aggregation

Front 35

Beta receptors

Back 35

Sympathetic

Beta 1 - s

Inc: HR, contractility, renin release, lipolysis

Beta 2 - s

Inc: vasodilation, bronchodilation, lipolysis, insulin release, aqueous humor production

Dec: uterine tone (tocolysis), ciliary muscle tone

Front 36

Muscarinic receptors

Back 36

Parasympathetic

M1 - q

CNA, enteric nervous system

M2 - i

Dec: HR and atrial contractility

M3 - q

Inc: exocrine gland secretions (lacrimal, salivary, gastric acid), gut peristalsis, bladder contraction, bronchoconstriction, pupillary sphincter contraction (miosis, ciliary muscle contraction (accommodation)

Front 37

Dopamine receptors

Back 37

D1 - s

Relaxes renal vascular smooth muscle

D2 - i

Modulates transmitter release, especially in brain

Front 38

Histamine receptors

Back 38

H1 - q

Inc: nasal bronchial mucus production, vascular permeability, contraction of bronchioles, pruritus, pain

H2 - s

Inc gastric acid secretion

Front 39

Vasopressin receptors

Back 39

V1 - q

Inc vascular smooth muscle contraction

V2 - s

Inc H2O permeability and reabsorption in collecting tubules of kidney

V2 is found in 2 kidneys

Front 40

What receptors use phospholipase C, protein kinase C, and Ca2+ in their pathways?

Back 40

H1, A1, V1, M1, M3 (Gq)

All Gq receptors follow this pathway

Front 41

What receptors use adenylyl cyclase, ATP, cAMP, and protein kinase A in their pathways?

Back 41

B1, B2, D1, H2, V2 (Gs)

M2, A2, D2 (Gi)

MAD 2's

All Gs and Gi receptors follow this pathway

Front 42

Back 42

Sea otters sleep holding paws so they don't drift apart at night

Just wanted to include all the images. Sorry this is small on phones.

Front 43

Back 43

Release of norepi from a sympathetic nerve ending is modulated by norepi itself, acting on presynaptic alpha-2 autoreceptors

Just wanted to include all the images. Sorry this is small on phones.

Front 44

Bethanechol

Category:

Clinical application:

Action:

Back 44

Category: cholinomimetic - direct agonist

Clinical application: postop ilius, neurogenic ileus, urinary retention

Action: activates bowel and bladder smooth muscle; resistant to AChE

Front 45

Carbachol

Category:

Clinical application:

Action:

Back 45

Category: cholinomimetic - direct agonist

Clinical application: constricts pupil, relieves intraocular pressure in glaucoma

Action: carbon copy of acetylcholine

Front 46

Methacholine

Category:

Clinical application:

Action:

Back 46

Category: cholinomimetic - direct agonist

Clinical application: Challenge test for asthma diagnosis

Action: methacholine stimulates muscarinic receptors of airways

Front 47

Pilocarpine

Category:

Clinical application:

Action:

Back 47

Category: cholinomimetic - direct agonist

Clinical application: potent stimulator of sweat, tears, and saliva; open- and closed-angle glaucoma

Action: Contracts ciliary eye muscles (open-angle), pupillary sphincter (closed-angle); resistant to AChE

"You cry, drool, and sweat on your pillow"

Front 48

Donepezil, galantamine, rivastigmine

Category:

Clinical application:

Action:

Back 48

Category: cholinomimetic - indirect agonist (anticholinesterase)

Clinical application: Alzheimer disease

Action: inc ACh

Front 49

Edrophonium

Category:

Clinical application:

Action:

Back 49

Category: cholinomimetic - indirect agonist (anticholinesterase)

Clinical application: historically used to dx myasthenia gravis (very short acting), but now MG diagnosed by anti-AChR Ab test

Action: inc ACh

Front 50

Neostigmine

Category:

Clinical application:

Action:

Back 50

Category: cholinomimetic - indirect agonist (anticholinesterase)

Clinical application: Postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postop)

Action: inc ACh

Neo CNS = no CNS penetration

Front 51

Physostigmine

Category:

Clinical application:

Action:

Back 51

Category: cholinomimetic - indirect agonist (anticholinesterase)

Clinical application: ACh toxicity; crosses blood-brain-barrier (CNS)

Action: inc ACh

Physostigmine phyxes atropine overdose

Front 52

Pyridostigmine

Category:

Clinical application:

Action:

Back 52

Category: cholinomimetic - indirect agonist (anticholinesterase)

Clinical application: Myasthenia gravis (long acting); doesn't penetrate CNS

Action: inc ACh; inc muscle strength

Pyridostigmine gets rid of myasthenia gravis

Front 53

Potential side-effect of cholinomimetics to watch for

Back 53

Cholinomimetics can cause exacerbation of COPD, asthma, and peptic ulcers

Front 54

Cholinesterase inhibitor poisoning

Back 54

Due to organophosphates that irreversibly inhibit AChE

Antidote: atropine (competitive inhibitor) + pralidoxime (regenerates AChE if given early)

DUMBBELSS

diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation

Front 55

Atropine, homatropine, tropicamide

Category:

Organ systems:

Clinical application:

Back 55

Category: muscarinic antagonist

Organ systems: Eye

Clinical applications: produce mydriasis and cycloplegia

Front 56

Benztropine

Category:

Organ systems:

Clinical application:

Back 56

Category: muscarinic antagonist

Organ systems: CNS

Clinical applications: Parkinson disease (park my Benz); acute dystonia

Front 57

Glycopyrrolate

Category:

Organ systems:

Clinical application:

Back 57

Category: muscarinic antagonist

Organ systems: GI, respiratory

Clinical applications:

Parenteral: preoperatively to reduce airway secretions

Oral: drooling, peptic ulcer

Front 58

Hyoscyamine, dicyclomine

Category:

Organ systems:

Clinical application:

Back 58

Category: muscarinic antagonist

Organ systems: GI

Clinical applications: antispasmodic for irritable bowel syndrome

Front 59

Ipratropium, tiotropium

Category:

Organ systems:

Clinical application:

Back 59

Category: muscarinic antagonist

Organ systems: respiratory

Clinical applications: COPD, asthma

I pray I can breathe soon!

Front 60

Oxybutynin, solifenacin, tolterodine

Category:

Organ systems:

Clinical application:

Back 60

Category: muscarinic antagonist

Organ systems: genitourinary

Clinical applications: reduce bladder spasms and urge urinary incontinence (overactive bladder)

Front 61

Scopolamine

Category:

Organ systems:

Clinical application:

Back 61

Category: muscarinic antagonist

Organ systems: CNS

Clinical applications: motion sickness

Front 62

Albuterol, salmeterol

Category:

Receptors effected:

Clinical application:

Back 62

Category: Sympatheticomimetic

Receptors effected: B2 > B1

Clinical application: Albuterol for acute asthma, salmeterol for long-term asthma or COPD

Front 63

Dobutamine

Category:

Receptors effected:

Clinical application:

Back 63

Category: Sympatheticomimetic

Receptors effected: B1 > B2, A

Clinical application: heart failure (inotropic > chronotropic), cardiac stress testing

Front 64

Dopamine

Category:

Receptors effected:

Clinical application:

Back 64

Category: Sympatheticomimetic

Receptors effected: D1 = D2 > B > A

Clinical application: unstable bradycardia, HF, shock

- Inotropic and chronotropic alpha effects predominate at high doses

Front 65

Epinephrine

Category:

Receptors effected:

Clinical application:

Back 65

Category: Sympatheticomimetic

Receptors effected: B > A

Clinical application: anaphylaxis, asthma, open-angle glaucoma

- Alpha effects predominate at high doses

- Significantly stronger effect at beta 2 receptor than norepi

Front 66

Isoprotenrenol

Category:

Receptors effected:

Clinical application:

Back 66

Category: Sympatheticomimetic

Receptors effected: B1 = B2

Clinical application: electrophysiologic evaluation of tachyarrhythmias

- Can worse ischemia

Front 67

Norepinephrine

Category:

Receptors effected:

Clinical application:

Back 67

Category: Sympatheticomimetic

Receptors effected: A1 > A2 > B1

Clinical application: hypotension (but dec renal perfusion)

- Weaker effect on beta 2 receptor than epi

Front 68

Phenylephrine

Category:

Receptors effected:

Clinical application:

Back 68

Category: Sympatheticomimetic

Receptors effected: A1 > A2

Clinical application: hypotension (vasoconstriction), ocular procedures (mydriatic), rhinitis (decongestant)

Front 69

Amphetamine

Category:

Mechanism:

Clinical application:

Back 69

Category: Indirect sympatheticomimetic

Mechanism: indirect general agonist, reuptake inhibitor, also releases stored catecholamines

Clinical application: narcolepsy, obesity, ADHD

Front 70

Cocaine

Category:

Mechanism:

Symptoms:

Back 70

Category: Indirect sympatheticomimetic

Mechanism: indirect general agonist, reuptake inhibitor

Symptoms: causes vasoconstriction and local anesthesia

Never give beta-blockers if cocaine intox suspected (can lead to unopposed alpha 1 activation and extreme HTN)

Front 71

Ephedrine

Category:

Mechanism:

Clinical application:

Back 71

Category: Indirect sympatheticomimetic

Mechanism: indirect general agonist, reuptake inhibitor, releases stored catecholamines

Clinical application: nasal decongestion, urinary incontinence, hypotension

Front 72

Norepinephrine vs. isoproterenol

Back 72

Norepinephrine inc􏰀 BP (alpha 1) but dec HR b/c inc 􏰂􏰀mean arterial pressure causes reflex bradycardia

Isoproterenol has little alpha effect but causes vasodilation (beta 2), resulting in dec 􏰁MAP and􏰀 inc HR through beta 1 and reflex activity

Front 73

Clonidine

Category:

Applications:

Toxicity:

Back 73

Category: Sympatholytic (alpha 2 agonist)

Applications: hypertensive urgency (limited situations); doesn't decrease renal blood flow

ADHD, Tourette syndrome

Toxicity: CNS depression, bradycardia, hypotension, respiratory depression, miosis

Front 74

Alpha-methyldopa

Category:

Applications:

Toxicity:

Back 74

Category: Sympatholytic (alpha 2 agonist)

Applications: HTN in pregnancy

Toxicity: direct Coombs positive hemolysis, SLE-like syndrome

Front 75

Non-selective alpha blockers

Applications:

Side effects:

Back 75

Phenoxybenzamine (irreversible)

Applications: pheochromocytoma (preoperative) to prevent catecholamine (hypertensive) crisis

Phentolamine (reversible)

Applications: give to patients on MAO inhibitors who eat tyramine-containing foods

Side effects: orthostatic hypotension, reflex tachycardia

Front 76

Alpha 1 selective blockers

Examples:

Applications:

Side effects:

Back 76

Examples: prazosin, terazosin, dexazosin, tamsulosin (all end in -osin)

Applications: urinary symptoms of BPH, PTSD (prazosin), HTN (except tamsulosin)

Side effects: 1st-dose orthostatic hypotension, dizziness, headache

Front 77

Alpha 2 selective blockers

Applications:

Side effects:

Back 77

Mirtazapine

Applications: depression

Side-effects: inc serum cholesterol and appetite

Front 78

Effect on blood pressure of alpha-blockade of epinephrine vs. phenylephrine

Back 78

Epinephrine

Initial response: increase BP (alpha response)

After alpha-block: decrease BP below normal (beta response)

Phenylephrine

Initial response: increase BP (alpha response)

After alpha-block: BP back to normal (not decreased like epi b/c it has no beta action)

Front 79

Beta-blocker application and effects

Back 79

Angina pectoris: dec HR and contractility, dec O2 consumption

MI: decrease mortality

SVT (metoprolol, esmolol): dec AV conduction velocity (class II antiarrhythmic)

HTN: dec cardiac output, dec renin secretion (beta 1 receptor blockade on JGA cells)

Heart failure: dec mortality in chronic HF

Glaucoma (timolol): dec secretion of aqueous humor

Front 80

Beta-blocker toxicity

Back 80

Impotence

Heart issues (bradycardia, AV block, HF)

CNS issues (seizures, sedation, sleep alterations)

Dyslipidemia (metoprolol)

Asthma/COPD exacerbations

Don't give with cocaine (unopposed alpha - HTN)

Still give to diabetics - don't worry about hypoglycemia b/c benefits outweigh risks

Front 81

Beta 1 selective antagonists

Back 81

Acebutolol, (partial agonist), atenolol, betaxolol, esmolol, metoprolol

Selective antagonists mostly go from A to M

Beta 1 with 1st 1/2 of alphabet

Front 82

Non-selective beta antagonists

Back 82

Nadolol, pindolol (partial agonist), propranolol, timolol

Non-selective antagonists mostly go from N to Z

Beta 2 with the 2nd 1/2 of the alphabet

Front 83

Non-selective alpha and beta antagnoists

Back 83

Carvedilol and labetalol

Non-selective alpha and beta antagonists have modified endings (-ilol and -atol instead of -olol)

Front 84

Nebivolol - what's special about it?

Back 84

Combines cardiac-selective beta 1 blockade with stimulation of beta 3 receptors, activating nitric oxide synthase in vasculature

Front 85

Study the list of specific antidotes and drug reactions from page 257 to 260 in First Aid 2015.

Back 85

It is too long of a list for flashcards. Sorry :(

Front 86

Drugs that cause.....

Vasospasm

Back 86

Cocaine, sumatriptan, ergot alkaloids

Front 87

Drugs that cause.....

Cutaneous flushing

Back 87

Vancomycin, adenosine, niacin, Ca2+ channel blockers

Vanc

Front 88

Drugs that cause.....

Dilated cardiomyopathy

Back 88

Anthacyclines (doxorubicin, daunorubicin)

Prevent with dexrazoxane

Front 89

Drugs that cause.....

Torsades de pointes

Back 89

Class II (solatol) and class IA (quinidine) antiarrhymics, macrolide antibiotics, antipsychotics, TCAs

Front 90

Drugs that cause.....

Adrenocortical insufficiency

Back 90

HPA surpression secondary to glucocorticoid withdrawal

Front 91

Drugs that cause.....

Hot flashes

Back 91

Tamoxifen, clomiphene

Front 92

Drugs that cause.....

Hyperglycemia

Back 92

Tacrolimus, protease inhibitors, niacin, HCTZ, corticosteroids

Taking pills necessitates having blood checked

Front 93

Drugs that cause.....

Hypothyroidism

Back 93

Lithium, amiodarone, sulfonamides

Front 94

Drugs that cause.....

Acute cholestatic hepatitis, jaundice

Back 94

Erythromycin

Front 95

Drugs that cause.....

Diarrhea

Back 95

Metformin, erythromycin, colchicine, orlistat, acarbose

Might excite colon on accident

Front 96

Drugs that cause.....

Focal to massive hepatic necrosis

Back 96

Halothane, amanita phalloides (death cap mushroom), valproic acid, acetaminophen

Liver HAVAc

Front 97

Drugs that cause.....

Hepatitis

Back 97

Rifampin, isoniazid, pyrazinamide, statins, fibrates

Front 98

Drugs that cause.....

Pancreatitis

Back 98

Didanosine, corticosteroids, alcohol, valproic acid, azathioprine, diuretics (furosemide, HCTZ)

Drugs causing a violent abdominal distress

Front 99

Drugs that cause.....

Pseudomembranous colitis

Back 99

Clindamycin, ampicillin, cephalosporins

Antibiotics predispose to superinfection by resistant C. difficile