Sileramram Usmle Pharm

Front 1

A lower Km means what for affinity of the enzyme?

Back 1

Increased
(Competitive inhibitors increase the Km)

Front 2

Competitive inhibitors do what to Vmax?

Back 2

Nothing

Front 3

Noncompetitive inhibitors do what to Vmax?

Back 3

Decrease

Front 4

Volume of distribution of a drug

Back 4

amount of drug in body/ plasma drug concentration

Front 5

Loading dose

Back 5

(target plasma concentration) x (volume of distribution/bioavailability)

bioavailability = 1 when drug is given IV

Front 6

maintenance dose

Back 6

Cp x CL/F

F= bioavailability

*maintenance dose changes for impaired renal and hepatic function

Front 7

Partial agonists do what to efficacy?

Back 7

decrease

Front 8

Where are nicotinic receptors found?

Back 8

skeletal muscle- neuromuscular junctions (Nm)

Autonomic ganglia (Nn)

Front 9

What kind of receptors are nicotinic receptors?

Back 9

Ligand-gated Na+/K+ channels

ACh

Front 10

What kind of receptors are Muscarinic ACh receptors?

Back 10

G-protein coupled

Front 11

Gq signals through what messenger?

Back 11

Phospholipase C --> PIP2 --> IP3 or DAG

IP3- increased Calicium
DAG- protein kinase C

Front 12

Which receptors signal through Gq?

Back 12

H1, alpha 1, V1, M1, M3

Front 13

Gs signals through what messenger?

Back 13

AC --> increased cAMP and Protein Kinase A

Front 14

Which receptors signal through Gs?

Back 14

Beta1, Beta 2, D1, H2, V2

Front 15

Gi signals through what messenger?

Back 15

BLOCKS AC --> decrease cAMP and protein A

Front 16

What receptors signal through Gi?

Back 16

M2, alpha 2, D2

Front 17

Name the major functions of alpha 1.

Back 17

1. Increased vascular smooth muscle contraction
2. Increased pupillary dilator muscle contraction (mydriasis)
3. Increased Intestinal and bladder sphincter muscle contraction

Front 18

Name the major functions of alpha 2.

Back 18

1. Decreased sympathetic flow
2. Decreased insulin release

Front 19

Name the major functions of beta 1.

Back 19

1. Increase heart rate
2. Increased contractility
3. Increased renin release
4. Increased lipolysis

Front 20

Name the major functions of beta 2.

Back 20

1. Vasodilation
2. Bronchodilation
3. Increased heart rate
4. Increased contractility
5. Increased lipolysis
6. Increased insulin release
7. Decreased uterine tone

Front 21

What are the major functions of M1?

Back 21

1. CNS
2. Enteric nervous system

Front 22

What are the major functions of M3?

Back 22

1. Increased exocrine gland secretion (sweat, gastric acid)
2. Increased gut peristalsis
3. Increased bladder contraction
4. Bronchoconstriction
5. miosis
6. ciliary muscle contraction (accommodation)

Front 23

What are the major functions of M2?

Back 23

Decreased heart rate and contractility of the atria

Front 24

D1?

Back 24

Relaxes renal vascular smooth muscle

Front 25

D2?

Back 25

Modulates transmitter release, mostly in brain

Front 26

V1?

Back 26

Increased vascular smooth muscle contraction

(V2 in kidney, water reabsorption)

Front 27

What is the mechanism of hemicholinium?

Back 27

blocks choline transporter presynaptically --> decreased ACh release

Front 28

Vesamicol mechanism?

Back 28

Blocks ACh packaging into VESicles to be released --> decreased ACh release

Front 29

Botulinum mechanism?

Back 29

Blocks releases of ACh

Front 30

Metyrosine mechanism?

Back 30

Blocks conversion of Tyr --> DOPA --> decreased NE release

Front 31

Reserpine mechanism?

Back 31

Blocks Dopamine packaging into vesicles

(like Vesamicol for cholinergic neurons)

Front 32

Guanethidine mechanism?

Back 32

Blocks release of NE.

Front 33

Amphetamine mechanism?

Back 33

Promotes release of NE. Blocks reuptake of NE too.

Front 34

Cocaine, TCA and amphetamine action in common?

Back 34

Blocks reuptake of NE.

Front 35

What are the three presynaptic receptors that modulate NE release?

Back 35

M2 -negative
AII- positive
alpha 2- Negative (NE negative feedback)

alpha 2- decreases sympathetic outflow via negative feedback

Front 36

Cholinomimetic agonists work through which receptors?

Back 36

Think M1, M2, M3 receptors

Front 37

Direct cholinomimetic agonists?

Back 37

Bethanechol- activates bowel and bladder
Carbachol- pupillary contraction, release of intraocular pressure, glaucoma
Pilocarpine- increases, sweat, tears and saliva, open and closed angle glaucoma
Methacoline- challenge test for asthma

Front 38

What are the two direct cholinomimetic agonists used in glaucoma

Back 38

Pilocarpine- open and closed
Carbachol

Front 39

What are the indirect cholinomimetic agonists (anticholinesterases)?

Back 39

Neostigmine- no CNS penetration, reverses postop neuromuscular blockade
Pyridostigmine- Myasthenia gravis, no CNS penetration
Edrophonium- Myasthenia gravis, short acting
Phyostigmine- glaucoma, atropine overdose, CNS PENETRANT
Echothiophate- glaucoma

Front 40

What are the two myasthenia gravis drugs?

Back 40

Pyridostigmine- long acting
Edrophonium- short acting

Front 41

What is the only anticholinesterase that crosses the blood brain barrier?

Back 41

Physostigmine- glaucoma and atropine overdose

Front 42

Symptoms of an anticholinesterase overdose?

Back 42

D-diarrhea
U-urination
M-miosis
B- bronchospasm
B- bradycardia
E- excitation of skeletal muscle and CNS
L- lacrimation
S- sweating and salivation

Front 43

Antimuscarinic for the eye?

Back 43

atropine
homatropine
tropicamide

- mydraisis, cycoplegia

Front 44

Antimuscarinic for parkinson's?

Back 44

benztropine

Front 45

Antimuscarinic for motion sickness?

Back 45

scopolamine

Front 46

Antimuscarinic for asthma and COPD?

Back 46

ipratroprium

Front 47

Antimuscarinic for urgency and mild cystitis?

Back 47

Oxybutynin
glycopyrrolate

-reduces bladder spasms

Front 48

Antimuscarinic for peptic ulcer treatment?

Back 48

Methscopolamine
pirenzepine
propantheline

- decreases secretion of acid (M3)

Front 49

Side effects of an antimuscarinic?

Back 49

Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat -cycloplegia- paralysis of ciliary muscle- loss of accomodation
Mad as a hatter- disoriented
constipation

acute angle-closure glaucoma
urinary retention in men with BPH
Hyperthermia- infants

Front 50

Hexamethonium mechanism?

Back 50

nicotinic antagonist

Use: ganglionic blocker, prevents vagal reflux response to changes in BP
- prevents reflex bradycardia caused by NE

Front 51

alpha 1+2, beta 1+2 agonist

Beta 1 mostly at low doses

Back 51

Epinephrine
- anaphylaxis, glaucoma (open angle), asthma, hypotension

Front 52

alpha 1 and alpha 2>beta2 agonist

Back 52

Norepinephrine
Use: hypotension with decreased renal profusion

Front 53

Stimulates both Beta1 and beta 2 equally

Back 53

Isoprotenerol
Use: AV block

Front 54

Stimulates D1=D2 and Beta>alpha

Back 54

Dobutamine
Use- shock, heart failure, cardiac stress testing
- ionotropic and chronotropic

Front 55

Stimulates alpha1> alpha 2

Back 55

Phenylephrine
Use: pupillary dilation, vasoconstriction, nasal decongestion

Front 56

Selective Beta 2 agonists

Back 56

Metaproterenol
Albuterol
Salmeterol
Terbulatine- reduces premature uterine contractions (Ritodrine too)

Front 57

Indirect sympathomimetics?

Back 57

1. Ampthetamine- releases stored catecholamines
2. Ephedrine- releases stored catecholamines
3. Cocaine- reuptake inhibitor

Front 58

Sympathomimetic that when given as a drug results in reflex bradycardia?

Back 58

norepinephrine
- usually increases heart rate and BP but as a drug can increase BP and decrease heart rate

Front 59

Drug that increases BP, pulse pressure and heart rate?

Back 59

Epinephrine

Front 60

Drug that decreases BP, pulse pressure and increases heart rate?

Back 60

Isoprotenerol- no alpha effects

Front 61

Centrally acting alpha 2 agonists?

Back 61

clonidine- hypertension
alpha- methyldopa

*especially in kidney disease because no decrease in blood flow to kidneys

Front 62

Nonselective alpha blockers used before removal of a pheochromocytoma?

Back 62

Phenoxybenzamine- irreversible
Phentolamine- reversible
- catecholamines released cannot overcome blockage

SE: orthostatic hyoptension, reflex tachycardia

Front 63

Alpha 1 selective blockers?

Back 63

Prazosin, terazosin, doxazosin
- end in -zosin
- use in hypertension, urinary retention in BPH

Front 64

Alpha 2 selective blocker?

Back 64

mirtazapine
Use- depression, decreases sympathetic outflow

Front 65

What happens to BP when Epi is administered after an alpha blockade?

Back 65

Reverse of before alpha blockade- decreased BP after blockade

Front 66

What happens to BP when phenylephrine is administered after an alpha blockade?

Back 66

Phenylephrine- alpha 1 > alpha 2
- usually increases BP
- Effect suppressed but no decrease

Front 67

What is the net Beta 2 agonist response for BP?

Back 67

decrease

Front 68

What is the net alpha response for BP?

Back 68

increase

Front 69

Which beta blockers have some alpha antagonism?

Back 69

carvedilol, labetalol

Front 70

Which beta blockers are nonselective?

Back 70

propranolol, timolol, nadolol, pindolol, labetalol

Front 71

Which beta blockers are selective for beta 1?

Back 71

Acebutolol, betaxolol, esmolol, atenolol, metoprolol

Front 72

Chlorpromazine is used for...

Back 72

nausea
- antiemetic

Front 73

What are the sulfa drugs?

Back 73

Celecoxib, furosemide, probenecid, thiazide, TMP-SMX, sulfasalazine, sulfonylureas, sumatriptan

Front 74

Antidote for amphetamine overdose?

Back 74

benzos and NH4Cl (acidifies the urine)

Front 75

Antidote for lead toxicity?

Back 75

CaEDTA, dimercaprol, succiner, penicillamine

Front 76

Antidote for methemoglobin toxicity?

Back 76

Methylene blue, vitamin C

Front 77

Antidote for heparin toxicity?

Back 77

protamine
- Works better for unfractionated heparin (IIa effects) rather than LMWH (not as good for Xa)

Front 78

Antidote for tPA, streptokinase

Back 78

Aminocaproic acid

Front 79

Antidote for Theophylline

Back 79

Beta-blocker

Front 80

Side effects of TCAs?

Back 80

Tri-Cs: Convulsions, Coma, Cardiotoxicity (arrhythmias)

Anticholinergic side effects- confusion etc

Tx: NaHCO3 for CV toxicity

Front 81

Two drugs that cause coronary vasospasm?

Back 81

Cocaine
Sumatriptan

Front 82

Four drugs that cause cutaneous flushing?

Back 82

VANC:
V- vancomycin
A- Adenosine
N- Niacin
C- Calcium channel blockers

Front 83

Two drugs associated with dilated cardiomyopathy?

Back 83

Doxorubicin (Adriamycin)
daunorubicin (chemotherapy for AML and ALL)

*Think dilated like a ruby

Front 84

What is cisapride used for?

Back 84

Increasing LES muscle tone in GERD
- prokinetic for gastroparesis

- 5HT4 receptor agonist

Front 85

Three drugs (or classes) that can cause torsades de pointes?

Back 85

III- sotalol - K channel blockers
IA- quinidine
Cisapride- 5HT4 agonist

Front 86

Drugs that cause agranulocytosis?

Back 86

1. Clozapine
2. Carbamazepine
3. Colchicine
4. Propylthiouracil
5. Methimazole (like propylthiouracil)
6. dapsone (in combo for PCP or malaria)- blocks bacterial synthesis of dihydrofolic acid

- antiepileptics, hyperthyroid treatment

Front 87

Drugs that cause aplastic anemia?

Back 87

1. Chloramphenicol
2. Benzene
3. NSAIDs
4. propylthiouracil
5. methimazole

Front 88

Toxicity of propylthiouracil or methimazole?

Back 88

1. Agranulocytosis
2. Aplastic anemia

Front 89

Direct Coombs-positive hemolytic anemia caused by what drug?

Back 89

Methyldopa
- caused by an immune process

Front 90

Cause of gray baby syndrome?

Back 90

Chloramphenicol

Front 91

Hemolysis in G6PD deficient patients caused by what drugs?

Back 91

1. Isoniazid
2. Sulfonamides
3. Primaquine
4. Aspirin
5. Ibuprofen
6. Nitrofurantoin (bacteriocidal)

Front 92

Drug causes of megaloblastic anemia?

Back 92

1. Phenytoin
2. Methotrexate
3. Sulfa drugs

Front 93

What is a substitute for ACE inhibitors that do not produce a cough?

Back 93

ARBs- losartan

Front 94

Drugs that cause Pulmonary fibrosis?

Back 94

1. Bleomycin - Hodgin's (ABVD), DNA strand breaker
2. Amiodarone
3. Busulfan- chemotherapy, alkylating agent

Front 95

Drug cause of hepatitis?

Back 95

Isoniazid

Front 96

Antibiotics that cause c.dif?

Back 96

Clindamycin, Ampicillin

Front 97

Drugs causing gynocomastia?

Back 97

1. Spironolactone
2. Digitalis
3. Cimetidine
4. Alcohol (chronic use)
5. estrogens
6. Ketoconazole

Front 98

Drugs that cause hot flashes?

Back 98

1. Tamoxifen
2. Clomiphene

Front 99

Drugs that cause hypothyroidism?

Back 99

1. Lithium
2. Amiodarone

Front 100

Drug that causes gingival hyperplasia?

Back 100

phenytoin

Front 101

Drugs that can cause gout?

Back 101

1. Furosemide
2. Thiazides
Hyper GLUC in serum (glucose, lipids, uric acid, calcium)

Front 102

Drugs that can cause osteoporosis?

Back 102

1. Corticosteroids
2. Heparin

Front 103

Drugs that cause photosensitivity?

Back 103

1. Sulfonamides
2. Amiodarone
3. Tetracyline

SAT for a photo

Front 104

Drugs that cause SLE like syndrome?

Back 104

1. Hydralazine
2. Isoniazid
3. Procainamide
4. Phenytoin

its not HIPP to have lupus

Front 105

Which antibiotic causes tendonitis, tendon rupture or cartilage damage in kids?

Back 105

Floroquinolones

Front 106

Which expired antibiotic can cause Fanconi's syndrome?

Back 106

Expired tetracycline
(also non expired cisplatin)

Front 107

What drugs can cause interstitial nephritis?

Back 107

Methicillin, NSAIDs, furosemide

Front 108

What drugs can cause symptoms of hearing loss, blurry vision and sweating?

Back 108

Cinchonism
- quinidine, quinine

Front 109

Drugs causes of diabetes insipidus?

Back 109

1. Lithium
2. Demeclocycline - tetracyline antibiotic

Front 110

Side effecst of isoniazid?

Back 110

1. Hemolysis in G6PD deficient patients
2. Hepatitis
3. SLE like syndrome
4. Seizures

Front 111

Drugs that cause ototoxicity?

Back 111

1. Aminoglycosides
2. Vancomycin
3. Loop diuretics
4. Cisplatin

Front 112

Quinidine's effect on P450?

Back 112

Induce and inhibit- induction more important

Front 113

St. John's wort effect on drug metabolism?

Back 113

Induces P450

Front 114

Barbiturates, Phenytoin, Rifampin, Carbamazepine and chronic alcohol use on drug metabolism?

Back 114

All are P450 inducers

Front 115

Grapefruit juice's effect on drug metabolism?

Back 115

Inhibits P450

Front 116

Sulfonamide effect on drug metabolism?

Back 116

Inhibits P450

Front 117

Acute alcohol use effect on P450?

Back 117

Inhibits

Front 118

Isoniazid, Cimetidine, Ketoconazole, Amiodarone, and erythromycin's effect on drug metabolism?

Back 118

P450 inhibitors

Front 119

Using disulfiram and drinking leads to what symptoms?

Back 119

Acetaldehyde build up- nausea, vomiting, headache, hypotension

Front 120

Salicylate toxicity can occur when the urine pH is changed in which way?

Back 120

acidifying urine (ie ammonium chloride) will decrease Salicylate clearance.

- acidify the urine to clear amphetamines (basic)

Front 121

Mechanism of ketoconazole?

Back 121

desmolase inhibitor- inhibits steroid synthesis

Front 122

Drug to block glucocorticoid action?

Back 122

Mifepristone (RU486)
- competitive inhibitor of progestins at progesterone receptor
- given with misoprostol (PGE1)

Front 123

Drug used in African Sleeping Sickness or for unwanted hairgrowth in PCOS?

Back 123

eflornithine

Front 124

benzodiazepine- date rape drug

Back 124

Flunitrazepam

Front 125

overdose- pinpoint pupils, seizures

Back 125

opioids

Front 126

"cold turkey" withdrawl

Back 126

opioids

Front 127

overdose- mydriasis

Back 127

- amphetamines
- cocaine
- LSD

Front 128

Hallucinogens?

Back 128

PCP- belligerence, impulsiveness, fear
LSD- hallucinations, flashbacks
Marijuana

Front 129

First sign of aspirin (salicylate toxicity)?

Back 129

tinnutus- can happen around 300 micrograms

hyperventilation and acidosis occur at higher doses

Front 130

Drug that prevents hemorrhagic cystitis with cylophosphamide or Ifosfamide?

Back 130

mesna- reactives with urotoxic metabolites of drugs

hemorrhagic cystitis from these drugs - no bacteria in urine, gross hematuria

Front 131

equation for half life?

Back 131

t1/2= (0.7 x Vd)/ Cl

Front 132

equation for maintenance dose? IV

Back 132

MD = Css x Cl

Front 133

equation for loading dose? IV

Back 133

LD = Cp x Vd

Front 134

Drugs that cause lithium toxicity

Back 134

Enhance absorption
- thiazides- Li follows Na reabsorption in proximal tubule
- NSAIDs

Front 135

Bosentan

Back 135

endothelin antagonist used in primary pulmonary hypertension

Front 136

cyproheptadine

Back 136

5HT receptor antagonist
- used in carcinoid syndrome

Front 137

-terol

Back 137

beta agonist; bronchodilator
albuterol; arformoterol; formoterol; levalbuterol; salmeterol

Front 138

Main effect of NO

Back 138

venodilation- decreased preload and cardiac work