Pharmacology 1

Front 1

Epinephrine

Back 1

increase heart rate, cardiac contractility, and blood pressure, decrease peripheral resistance

Front 2

Phenylephrine

Back 2

decongestant of mucous membranes, Treatment of Hypotension and autonomic insufficiency, causes Mydrasis: contraction of radial muscle of iris, α-Receptor Agonists

Front 3

Clondine

Back 3

α2-Receptor Agonists, works on hypothalamus to reduce sympathetic drive, withdrawal from addiction

Front 4

Dipivefrin

Back 4

prodrug for epi, have Beta 2 action to increase outflow of aqueous humor, and Alpha 2 action of decrease production of aqueous humor

Front 5

isoproterenol

Back 5

strongly increase heart rate, increases cardiac contractility, and systolic blood pressure, strongly decrease peripheral resistance

Front 6

Beta 2 agonists

Back 6

Bronchial smooth muscle dilator
e.g. albuterol salmeterol

Front 7

dobutamine

Back 7

Used to treat circulatory shock because it increase cardiac output with increasing peripheral resistance

Front 8

dopamine

Back 8

increase cardiac output and activates dopamine receptor on kidneys, intestines, and other abdominal organs increasing blood flow without decreasing blood pressure

Front 9

propranolol

Back 9

Binds to b1- and b2-receptors with equal affinities
decrease heart rate, cardiac output (and corresponding increase p.r.)
decrease blood flow to most tissues
over long term decrease in blood pressure (but no postural hypotension)

Front 10

metoprolol, atenolol, esmolol

Back 10

β1-selective antagonists

Front 11

pindolol

Back 11

b-Receptor Antagonists with Intrinsic Sympathomimetic Activity

Front 12

third generation beta-blockers: labetolol, carvedilol

Back 12

labetolol blocks b1, b2, and a1-receptors; exhibits ISA at b2-receptors -used for hypertension and hypertensive emergencies
carvedilol blocks b1, b2, and a1-receptors-exhibits exhibits unique antioxidant and antiproliferative properties
-numerous clinical trials indicate that carvedilol improves ventricular function and reduces mortality/morbidity in mild-to-severe congestive heart failure

Front 13

α1-selective antagonists: terazosin, doxazosin, tamsulosin

Back 13

Prominent cardiovascular effects:
increase blood flow to most tissues
decreaseblood pressure without tachycardia

Front 14

sumatriptan

Back 14

5HT1D (and 5HT1B) receptor agonists
used for treatment of migraines

Front 15

atropine

Back 15

Tertiary amine: can enter CNS
Eye: mydriasis and cycloplegia
GI tract: block contractions and secretions
Blocks sweat formation
Prototype of Antimuscarinic agents
Atropine flush: dilation of facial blood vessels
Mild tachycardia
Marginal effect on blood pressure

Front 16

scopolamine

Back 16

Scopolamine exerts more CNS action than atropine drowsiness and amnesia

Front 17

ipratropium nicotine

Back 17

Quaternary amine
Administered by inhalation in reversible airway disease where bronchial constriction has resulted from increased parasympathetic stimulation

Front 18

trimethaphan

Back 18

GANGLIONIC BLOCKERS
Very short acting: rapidly metabolized by plasma ChE and is administered continuously by IV infusion

Front 19

D-tubocurarine (curare)

Back 19

Competitive or Nondepolarizing Blocking Drugs paralyzes skeletal muscles at high doses disrupt transmission at autonomic ganglia
enhanced by general anesthetics (enflurane, isoflurane, and, to a lesser extent, halothane) and by some antibiotics (neomycin, streptomycin, and tetracyclines)

Front 20

atracurium

Back 20

Use of d-tubocurarine replaced by shorter acting competitive NMJ nAChR blockers

Front 21

succinylcholine

Back 21

persistent depolarization at NMJ endplate
Very rapid and brief * (unless you’re the wrong genotype)
skeletal muscle paralysis within 1 min of IV admin.
recovery within 5 min of IV admin

Front 22

methacholine

Back 22

Methacholine also has a longer duration of action than acetylcholine because it resists hydrolysis by plasma cholinesterases and is hydrolyzed by acetylcholinesterase at only one-third the rate that acetylcholine is.
Physicians occasionally use methacholine diagnostically to test for bronchial hyperactivity and asthmatic conditions.

Front 23

carbachol

Back 23

Carbachol has a long duration of action (2-3 hours) because the carbamate substitution protects it from hydrolysis by either acetylcholinesterase or plasma cholinesterases.
Carbachol has been used topically in the eye to manage glaucoma. It acts on muscarinic cholinergic receptors of the sphincter and ciliary muscles to produce miosis, thereby opening the canals of Schlemm to ease the outflow of aqueous humor and decreasing intraocular pressure.

Front 24

bethanechol

Back 24

When given orally or s.c. in the usual doses, bethanechol exerts only mild cardiovascular effects and affects mainly the gastrointestinal tract and urinary bladder.
Physicians sometimes prescribe bethanechol to increase tone and contractions of a patient’s intestine and urinary bladder.

Front 25

pilocarpine

Back 25

Pilocarpine is a natural plant alkaloid that exhibits primarily muscarinic receptor agonist actions
Since it is not a choline ester, it is not a substrate for cholinesterases and has a duration of action of 2-3 hours
Pilocarpine is often used topically in the eye to manage glaucoma. Like carbachol, it produces contraction of the iris ciliary and sphincter muscles to facilitate outflow of aqueous humor.

Front 26

edrophonium

Back 26

REVERSIBLE CHOLINESTERASE INHIBITORS
Quaternary alcohol
Short duration of action
Edrophonium tests
diagnosis
adjust dose of anticholinesterase
for MYASTHENIA GRAVIS

Front 27

neostigmine

Back 27

Carbamate esters: these drugs serve as substrates for AChE
Quaternary amine (charged – not enter brain)
Stimulates GI contractions and secretions and urinary bladder
contractions
Improves neurotransmission at NMJ

Therapeutic Uses:
nonobstructive intestinal and urinary bladder
Myasthenia gravis

Front 28

DFP

Back 28

Organophosphate cholinesterase inhibitors:these drugs phosphorylate AChE and can irreversible inactivate the enzyme
of these drugs can be used in the treatment of glaucoma BUT, as last resort, with long term use, these drugs can cause cataracts

Front 29

COMT inhibitors

Back 29

COMT is important for termination of the physiological action of epinephrine
tolcapone (Tasmar) and entacapone (Comtan) are COMT inhibitors used clinically during treatment of Parkinson’s disease with L-DOPA

Front 30

MAO inhibitors

Back 30

MAO in intestinal mucosa and liver protects the body from phenylethylamines found in high amounts in food and produced by intestinal bacteria
MAO inhibitors were the first important antidepressant drugs---their mechanism of action involves elevation of neurotransmitter (NE and serotonin) levels in the brain

Front 31

cocaine, tricyclic antidepressants

Back 31

Competitive Antagonists of the NE Transporter on Sympathetic Nerve Endings

Front 32

tyramine

Back 32

all action due to release of NE
tyramine “displaces” NE from sympathethetic nerve endings to produce sympathomimetic effects, particularly vasoconstriction

Front 33

amphetamine

Back 33

works the same way tyramine does

Front 34

reserpine

Back 34

Vesicular uptake of dopamine and norepinephrine and depletion of NE by pharmacological inhibition of the vesicle uptake mechanism