5.11 General Pharmacology

Front 1

Competetive Enzyme inhibitors affect Km or Vmax?

Noncompetitive Enzyme inhibitors affect Km or Vmax?

Back 1

Competitive change the affinity of the substrate for the enzyme; change Km

Noncompetitive changes the ability of the ezyme to work, change Vmax

Front 2

Correlate Km with enzyme/substrate affinity?

Back 2

↓Km / ↑affinity

Front 3

What is Vd?

What does a high Vd mean?
A low Vd?

Back 3

Vd= amt of drug in body/amt of drug in vasculature

high Vd: drug primarily in tissues
low Vd: drug primarily in vasculature

Front 4

How many half lives for a drug to reach steady state?

Back 4

3-5

Front 5

What route of drug administration makes bioavailability = 1?

What route of drug administration makes bioavailability not = 1?

Back 5

bio=1: IV

bio not 1: oral

Front 6

What is the difference between Zero Order Elimination and First order elimination?

Back 6

Zero: constant RATE of removal

First: constant FRACTION of removal

Front 7

Couple drugs that use Zero Order elimination?

Back 7

1. ASA
2. Ethanol

Front 8

Weak acids get trapped in the renal tubules in what types of environment?

Weak bases get trapped in renal tubules in what type of environment?

HINTS: Draw out the dissociation equations.

Back 8

Weak acids: trapped in basic environments

Weak bases: trapped in acidic environments

Front 9

How does liver metabolism change the hydrophobicity of drugs?

Back 9

drugs become increasingly more polar as they are metabolized.

Front 10

What is the general functions of Phase I and Phase II liver metabolism?

Back 10

Phase I is CytP450
Phase II is conjugation

Front 11

How does a competitive antagonist change the ED50 of a drug?

How does a non-competitive antagonist change the ED50 of a drug?

Back 11

competitive increases the ED50 (shifts to the right because more drug can overcome the effects)

non-competitive keeps the ED50 the same

Front 12

What is the therapeutic index?

Back 12

LD50/ED50

Front 13

Describe the G protein class mechanisms? (3)

Back 13

s: ↑AC → ↑cAMP → ↑PKA

q: ↑PLC → ↑IP3(Ca+2) + DAG(PKC)

i: ↓AC → ↓cAMP → ↓PKA

Front 14

1. What GCPR is responsible for renal vascular dilation?

2. What GCPR is responsible for ↑gastric secretions?

3. Which GCPR are responsible for miosis and mydriasis?

Back 14

1. D1

2. H2

3. mydriasis: α1/miosis: M3

Front 15

1. Which GCPR is responsible for modulating neurotransmitter release in the brain?

2. Which GCPR is responsible for increasing water permeability in the kidney?

3. Which GCPR is responsible for releasing renin?

Back 15

1. D2

2. V2

3. B1

Front 16

Compare the mechanisms of muscarinic cholinergic and nicotinic cholingergic receptors?

Back 16

muscarinic: GPCR

nicotinic: K/Na+ ligand gated

Front 17

How does amphetamine and cocaine MOAs differ?

Back 17

amphetamine causes increased release of NT from terminals

cocaine causes decreased reuptake of NT into terminals

Front 18

What is the etiology of Myasthenia Gravis?

What are the two drugs used with Myasthenia gravis and their functions?

Back 18

Abs to Ach receptors

eDrophonium=diagnoses it
pyRIDostigmine=gets RID of it

Front 19

Functions of:
1. benztropine
2. scopolamine
3. ipratropium
4. glycopyrrolate
5. methscopolamine

Back 19

1. Parkinsons
2. Motion Sickness
3. Asthma, COPD
4. GU spasm
5. peptic ulcer

Front 20

Why does a muscarinic antagonist cause an increase in body temperature?

Back 20

prevents the sympathetic/cholinergic act of sweating to reduce body temperature

Front 21

What are the non-selective adrenergic antagnonists? (2)

Back 21

1. carvedilol
2. labetalol

Front 22

What are the partial B-agonist drugs? (2)

Back 22

1. pindolol
2. acebutolol

Front 23

What are two antidotes for organophosphate poisoning and their mechanisms? (2)

Back 23

1. pralidoxime (saves the AChE)
2. atropine (blocks the mACh receptor)

Front 24

What is the antidote for amphetamine toxicitiy?

Back 24

NH4Cl (acidify the urine)

Front 25

What is the antidote for B-blocker toxicitiy?

Back 25

glucagon: because it will stimulate cAMP independently of the B-receptors

Front 26

What is the antidote to copper, arsenic and gold toxicitiy?

Back 26

penacillamine

Front 27

What is the antidote to methemoglobin toxicity?

Back 27

Methylene blue

Front 28

What is the antidote to TCA toxicity?

Back 28

HCO3-, alkalinize the urine

Front 29

What is the antidote for heparin toxicity?

What is the antidote of warfarin toxicity?

Back 29

heparin: protamine sulfate (highly positive binds highly negative heparin)

warfarin: K+

Front 30

What is the antidote for tPA or streptokinase toxicity?

Back 30

aminocaproic acid

Front 31

What is the antidote for theophylline toxicity?

Back 31

B-blockers

Front 32

What is the antidote for lead poisoning?

What are the S/S? (4)

Back 32

Succimer

LEAD
Lead Lines in gums
Encephalopathy
Anemia
Dropped Wrists/Foot

Front 33

Two drugs most often known for causing pseudomembranous colitis? (2)

What drug is synonymous with gray baby syndrome?

Back 33

1. ampicillin
2. clindamycin

chloramphenicol

Front 34

INH side effect?

Which commonly prescribed drug class causes coughing?

Back 34

hepatitis

ACE inhibitors

Front 35

Which drugs incite hemolysis in G6-PD deficient patients? (6)

Back 35

IS PAIN
INH
sulfa
primaquine
ASA
Ibu
Nitrofurantoin

Front 36

What drugs cause megaloblastic anemia? (3)

Back 36

having a BLAST with PMS:
Phenytoin
MTX
Sulfa

Front 37

Which drugs are known to cause gout? (2)

Which drug is most known for Stevens Johnson syndrome?

Back 37

diuretics:
1. furosemides
2. thiazides

Lamotrigine

Front 38

Which drugs are known for inciting SLE? (2)

What is Fanconi's syndrome and the drug that tends to cause it?

Back 38

procainamide, hydralazine

disrupted proximal kidney tubules; expired tetracycline

Front 39

Two drugs that can cause DI? (2)

Drug that causes Cinchonism?

Back 39

1. lithium
2. demeclocycline

quinine/quinidine

Front 40

What drugs cause disulfiram interactions? (2)

Back 40

1. 2nd generation cephalosporins
2. metronidazole

Front 41

What are the primary drugs that are Cyp inducers?

What are the primary drugs that are Cyp inhibitors?

Back 41

Queen Barb Griesemer Rapidly Steals Car Phenders: Quinidine Barbiturates Grisefulvin St. Johns, Rifampin, Carbamezapine, Phenytoin

SICkEG
sulfonamides, INH, cimetidine, ketoconazole, erythromycin, grapefruit juice

Front 42

When considering different alcohol toxicities, what does methanol cause? What does ethylene glycol cause?

What is the initial enzyme that detoxifies these?

What enzyme does disulfiram inhibit?

Back 42

ethylene glycol: kidney damage
methanol: retinal damage

initial enzyme: alcohol dehydrogenase

disufiram: acetaldehyde dehydrogenase

Front 43

1. -etine
2. -ipramine
3. -tropin
4. -zosin
5. -tidine
6. -triptan

Back 43

1. SSRI
2. TCA
3. pituitary hormone
4. alpha antagonist
5. H2 antagonist
6. 5-HT(1A) agonist