Kaplan: Pharm - Autonomic Drugs

Front 1

Hydrocarbons from smoking (induce/inhibit) 1A2?

This (increases/decreases) the number of 1A2 NZs in a smoker?

Back 1

Induce

Increases

Front 2

General CYP 3A4 inducers:

Back 2

"Smoking & Drinking in Barb's Car Rif's her Phen"

Chronic Smoking & Alcohol
Anticonvulsants (Barbiturates, carbamazapine, phenytoin)
*Rifampin*
Glucocorticoids

Front 3

Inhibitors of CYP 3A4:

Back 3

"COKE & Grapefruit w/ your PI"

Cimetidine
Omeprazole
ketoconazole
erythromycin
Grapefruit juice
Protease inhibitors

Front 4

3 Drugs w/ zero order elimination

Back 4

Ethanol, phenytoin, salicylates

All have zero-order kinetics only at high doses. Zero order kinetics occur when elimination mechanisms are saturated (reached Vmax).

Front 5

Receptors linked to Gs proteins

Action on cAMP?

Back 5

All beta, D1, glucagon, H2, prostacyclin, some 5-HT

All increase cAMP production --> activation of PKA

Front 6

Receptors linked to Gi protiens?

Action on cAMP?

Back 6

alpha-2, M2, D2, several opioid and 5-HT

All decrease cAMP production --> inhibition of PKA

Front 7

Receptors linked to Gq proteins?

Action?

Back 7

M1, M3, alpha-1, angiotensin II, several 5-HT

Action: Activation of phospholipase C -> activation of PKC

Front 8

Bethanechol

Back 8

Class: Muscarinic Agonist

AChE hyrdolysis: (-)

Rx: post-op/neurogenic (non-obstructive!) ileus, urinary retentions --> Decreases GI/GU activity

Front 9

Pilocarpine

Back 9

Muscarinic Agonist

Rx: Glaucoma (topical), xerostomia (oral)

Front 10

Methacholine

Back 10

Muscarinic Agonist

Activity: M > N

Use: "Methacholine challenge test" to Dx asthma

Front 11

Muscarinic Agonists (4)

Back 11

Acetylcholine (endogenous)
Bethanechol
Pilocarpine
Methacholine

Front 12

Edrophonium

Back 12

AChE inhibitor (short-acting)

Use: Dx of myasthenia gravis --> differentiate between myasthenia (too little ACh) from cholinergic crisis (too much ACh)

Front 13

Physostigmine

Back 13

AChE inhibitor (intermediate acting)

PK: crosses BBB

Rx: Glaucoma; **antidote in atropine OD (stops central & peripheral effects)**

Front 14

Neostigmine
Pyridostigmine

Back 14

AChE inhibitor (intermediate acting)

PK: Don't cross BBB

Use: urinary retention (alt to bethanechol)
Tx for myasthenia
reversal of nondepolarizing NM blockers

Front 15

Donepezil
(tacrine)

Back 15

AChE inhibitor

PK: cross BBB

Rx: Alheimer Dz (slows loss of cholinergic neurons)

Front 16

Organophosphates

Back 16

AChE inhibitors

PK: Irreversible inhibitors!

Use: Echothiophate used in glaucoma Tx
Commonly used in pesticides (malathoin, parathoin) and nerve gas (sarin)

Front 17

Atropine

Back 17

Muscarinic receptor agonist

PK: Enters CNS

Sx: Muscarinic activation (esp. hyperthermia w/ resulting vasodilation --> kills kids; tachycardia --> Tx w/ AV block)

Front 18

Non-automomic drugs w/ antimuscarinic properties

Back 18

Antihistamines (1st generation only)
Tricyclic antidepressants
Antipsychotics
Quinidine
Amantadine (Parkinsonism Tx)
Meperidine (Only opioid that doesn't get miosis)

Front 19

Tx of acute atropine toxicity

Back 19

Symptomatic support
&
Physostigmine (b/c it has CNS activity)

Front 20

Tropicamide

Back 20

M antagonist

Use: ophthalmologic (topical)

Front 21

Ipratropium

Back 21

M antagonist

Use: Asthma and COPD (inhalation)

*no CNS entry*

Front 22

Scopalamine

Back 22

M Blocker

Use: Motion sickness (causes sedation and anterograde amnesia)

Front 23

Benztropine,
Trihexyphenidyl

Back 23

M Blocker

PK: CNS entry

Use: Parkinsonism,
acute extrapyramidal Sx from antipsychotics

Front 24

*Oyxbutyrin*
Tolterodine

Back 24

M Blocker

Use: urinary incontinence

Front 25

Hexamethonium

Back 25

Nicotinic ganglion blocker

Front 26

Mecamylamine

Back 26

Nicotinic ganglion blocker

Front 27

Phenylephrine

Back 27

alpha-1 agonist

Use: nasal decongestant,
ophthalmologic use (mydriasis w/o cyclopegia), prostate

Front 28

Methoxamine

Back 28

alpha-1 agonist

Use: paroxysmal atrial tachycardia via vagal reflex (uses reflex activity)

Front 29

Clonidine

Back 29

alpha-2 agonist

Use: mild-moderate HTN (decrease TPR),
Opiate withdrawal

DDI: Tricyclic ADs decrease efficacy of A2 agonists



Memory: "alpha = MC2"

Front 30

Methyldopa

Back 30

Alpha-2 agonist

Use: mild-moderate HTN, esp in pregnancy

SE: Hemolytic anemia - (+) Coombs test,

DDI: Tricyclic ADs decrease efficacy of A2 agonists

Front 31

Isoproterenol

Back 31

Non-selective Beta agonist

Use: Bronchospam, heart block, bradyarrhythmias

SE: flushing, angina, arrhythmias

*Note: don't confuse w/ metaproterenol, a B2 agonist!

Front 32

Dobutamine

Back 32

Beta agonist (B1 > B2)

Use: CHF

Front 33

Salmeterol
albuterol

Back 33

B2 agonist

Use: Asthma

Front 34

Terbutaline

Back 34

B2 agonist

Use: Asthma

Front 35

Ritodrine

Back 35

B2 agonist

Use: premature labor

Front 36

Epinephrine

Back 36

Low dose: B1, B2 stimulation
Effect = Isoproterenol

High dose: a1 predominates --> vasoconstriction --> increase BP --> decrease HR
(Effect = NE)

Use: DOC for anaphylaxis, asthma, cardiac arrest

Front 37

Norepinephrine

Back 37

Stimulation of a1, B1 (on organ), a2 (on nerve)

Initially increases HR, then decreases HR long-term

Front 38

How do you distinguish NE from Epi?

Back 38

Epinephrine reversal:

NE or Epi alone = HTN
NE + a1 blocker = normotensive
Epi + a1 blocker = hypotension

Front 39

Phentolamine

Back 39

Alpha receptor antagonist (non-selective, competitive)

Use: HTN, Pheochromocytoma

Front 40

Phenoxybenzamine

Back 40

Alpha receptor antagonist (non-selective, noncompetitive/irreversible)

Use: HTN, Pheochromocytoma

Front 41

Prazosin
doxazosin
Terazosin
Tamulosin

Back 41

a1 blockers

Use: HTN, BPH

Front 42

Yohimbine

Back 42

Selective a2 blocker

Use: Orthostatic hypotension,
impotence

Front 43

Mirtazapine

Back 43

Selective a2 blocker

Use: antidepressant
(Unique MOA for an antidepressant! --> inhibits an inhibitory action)

Front 44

Acebutolol, atenolol, metorolol

Any "-olol" that starts w/ A-M; BEAM

Back 44

Selective B1 blocker

Notes: B1 selective for heart
Safer for asthma and diabetes patients

PK: Atenolol has no CNS entry

Use: Stable/Classic angina (CI in vasospastic angina)
HTN
post-MI

Front 45

Which Beta blockers are used as antiarrhythmetics?

Back 45

Class II BB:

propranolol, acebutolol, esmolol

Front 46

Pindolol, Propranolol, Timolol

Any "-olol" that starts w/ N-Z

Back 46

Nonselective beta blocker

Notes: May have effects on bronchospasm, vasospasm, etc
- More sedative effects

Front 47

Which two beta blockers have ISA activity and do not increase blood lipids?

Back 47

Acebutolol and Pindolol

Front 48

Labetalol

Back 48

Combined a1 and BB activity

Use: CHF

Front 49

Carvedilol

Back 49

Combined a1 and BB activity

Use: CHF
- Class/stable angina (clinically same as isosorbide)

"-olol" = BB only
"-alol" or "-ilol" = BB + something else

Front 50

Sotalol

Back 50

Combined K-channel blocker and BB activity

Use: antiarrhythmetic (class III)

Front 51

Use of pilocarpine in glaucoma

Back 51

Drug class: Cholinomimetic

Activation of M receptor
contraction of ciliary muscle
increases flow through the canal of Schlemm

Front 52

Use of echothiophate in glaucoma

Back 52

AChE inhibitor

Increases outflow of fluid

Front 53

Use of timolol in glaucoma

Back 53

Class: Beta Blocker

Blocks actions of NE at ciliary epithelium --> decreases aqueous humor formation

Front 54

Use of acetazolamide in glaucoma

Back 54

Class: Carbonic anhydrase inhibitor

Decreases aqueous humor formation

Front 55

Use of mannitol in glaucoma

Back 55

Class: Osmotic

Increases outflow of fluid