Exam 1: Bolded Drugs

Front 1

Hemicholinium (HC-3)

Back 1

blocks transport of choline & consequently will eventually cause an inhibition of cholinergic function.
*Since choline (one of the building blocks of ACh is not synthesized in the nerve, it must be pumped into the nerve. So if HC-3 blocks that from happening it inhibits ACh synthesis and therefore function.

Front 2

Acetylcholine

Back 2

-Choline Ester
-Must be injected to have effect.
-Intravenous short term stimulation b/c broken down by cholinesterase.
-lacks receptor specificity.
-Not used therapeutically.

Front 3

Bethanechol

Back 3

-Choline Ester
-only choline ester with well established clinical use.
-has mostly MUSCARINIC STIMULATION EFFECT.
-treats post op urinary retention and atony of GI tract.

Front 4

Nicotine

Back 4

-Naturally occuring cholinergic stimulants (alkaloids)
-Stimulates all nicotinic receptors.
-if injected: stimulate all autonomic ganglia and skeletal muscle endplate nicotinic receptors.

Front 5

Muscarine

Back 5

-Naturally Occuring
-rapid-onset mushroom poisoning: give antidote ATROPINE = prognosis good.
-delayed onset poisoning: poorer prognosis.
-muscarine will stimulate all muscarinic receptors whether innervated or non-innervated.

Front 6

Pilocarpine

Back 6

-Naturally occurring
-south american shrub
-selectively activates MUSCARINIC receptors
-not as highly charged so crosses the membrane barrier readily.
-treats GLAUCOMA: increase aqueous flow and widens angle.

Front 7

Physostigmine

Back 7

-Anticholinesterase agent
-reversible agent
-isolated from Carabar bean
-topical treatment for GLAUCOMA.
-most rational agent for Tx of ATROPINE POISONING.
-treat BRAIN DAMAGE
*tertiary, not as highly charged, cross barrier better*

Front 8

Pyridostigmine

Back 8

-treat MYASTHENIA GRAVIS
-other agents maybe tolerated better b/c of this agents potency.

Front 9

Donepezil & Tacrine

Back 9

-CNS acting anticholinesterase drugs
-treat COGNITIVE DYSFUNCTION IN ALZHEIMER'S DISEASE.

Front 10

Parathion:

Back 10

-Anticholinesterase Agent
-irreversible agent
-common insecticides used in agriculture.
-not itself anti AChase but converted by LIVER into active agent: PARAOXON.

Front 11

Atropine

Back 11

-Muscarinic blocking drug
-long lasting (1 week -10 days)
-absorbed readily through oral admin.
-CNS excitation
-toxic to children
-poisoning: hot dry skin, dilated pupil, maniacal behavior
-Loss of bladder tone

Front 12

Scopolamine

Back 12

-Muscarinic blocking drug
-CNS depressant
-patch applied to back of neck for motion sickness and throwing up.

Front 13

Tropicamide

Back 13

Muscarinic blocking drug
-less potent and much shorter acting muscarinic antagonist
-more useful for general opthalmological exams than atropine and scopolamine.

Front 14

Ipratropium

Back 14

-Muscarinic blocking drug
-quaternary amine: fewer systemic (esp. CNS) effects.
-applied topically to airway via INHALER.
-treat COPD- produces bronchoodilation.
-2nd-line drug for treatment of bronchial asthma.

Front 15

Benztropine

Back 15

-muscarinic blocking drug
-CNS acting antimuscarinic drug
-relieve symptoms of Parkinson's

Front 16

Oxybutynin

Back 16

-muscarinic blocking drug
-Atropine like agent
-treat SPASMS OF BLADDER seen after urologic surgery and in some neurological disorders producing bladder hyperactivity.
-orally or topically (catheter)
-decreases tone of bladder smooth muscle=improves continence.

Front 17

Cholinomimetics

Back 17

-Paralytic ileus
-Atony of bladder
-Glaucoma
-Nicotine Addiction
-Myasthenia Gravis
-Toxicological considerations
-Dementia

Front 18

Cholinergic Antagonists

Back 18

-Ophthalmic exams
-Bladder hyperactivity
-Cardiac effects
-bronchodilator
-motion sickness
-Parkinsonism
-Toxicological considerations

Front 19

EPI

Back 19

-Acts on all alpha and beta receptors.
-not effective given orally.
-injected- short life.

Front 20

Cardiovascular effect of EPI

Back 20

-alpha: induced vasoconstriction.
-beta: induced vasodilation.

Front 21

EPI on heart:

Back 21

-Beta 1: increase HR and contractility.
*change in CO not sufficient to overcome effect on blood vessels*

Front 22

EPI on Beta 2:

Back 22

-relax bronchial smooth muscle in asthma treatment and bronchospasm in anaphylactic shock.

Front 23

EPI on metabolism (fight or flight):

Back 23

Beta receptors: increase adenlate cyclase activity to form cAMP second messenger causing:
-increase plasma glucose by liver glycogen breakdown
-inhibits glycogen synthesis.
-stimulates gluconegenesis
-breaks down fat into fatty acids

Front 24

NE

Back 24

-not orally effective, parenterally short activity.
-acts on all alpha and only beta 1.
-not clinically useful

Front 25

Dopamine (DA)

Back 25

-precursor to NE and EPI
-CNS: important NT, esp. in extrapyramidal motor system.
-treat parkinson's

Front 26

DA on renal blood vessels

Back 26

-non-innervated dopamine receptors.
-produce vasodilation.
treat certain shock stages.

Front 27

DA high doses:

Back 27

stimulate both alpha and beta receptors
Increase BP and CO.

Front 28

Amphetamine and meth:

Back 28

-Non-cat. sympamim.
-alpha agonist
-indirect, orally effective
-readily enters CNS
-increases mood and appetite suppression.
-tolerance develops rapidly.
-rebound depression frequently develops.
-ED50 increases, LD50 stays same due to tolerance.
-lead to cerebral hemorrhage and intense vasoconstriction of CNS vessels.

Front 29

clinical uses of Amphetamine:

Back 29

1. hyperkinetic children: become more sedate, increase attention span
2. narcolepsy

Front 30

Methylphenidate

Back 30

-mild CNS stimulant
-Alpha agonist
-large doses: CNS excitation=convulsions
-RITALIN-ADD, ADHD
-good oral bioavailability.

Front 31

Ephedrine

Back 31

-Alpha agonist
-1/2: direct stimulation on all alpha and beta.
-1/2: indirect: releases NE from neural stores.
-oral treatment for bronchial asthma (B effect)
-ear and nasal decongestion
-mydriasis w/o cycloplegia (A effect)

Front 32

Phenylephrine

Back 32

-Alpha agonist
-presser agent and produce mydriasis
-nasal spray- local vasoconstriction but causes rebound congestion.

Front 33

Clonidine:

Back 33

-Alpha agonist
-alpha 2: long term stimulation of CNS=decreases symp. tonic activity from brain.
-treat high BP
-decrease brain neuron activity involved with pain. (analgesic)

Front 34

Terbutaline

Back 34

-B-agonist
-modification of metaproterenol
-longer acting than metaproterenol but higher incidence of cardiac side effects
-PREVENT PREMATURE CHILDBIRTH.

Front 35

Albuterol

Back 35

-B-agonist
-treats ASTHMA (similar to terbutaline)
-longer acting but with fewer cardiac side effects than terbutaline

Front 36

Salmeterol

Back 36

-B-agonist
-long-acting Beta 2 agonist.
-treats BRONCHIAL ASTHMA

Front 37

Ritodrine

Back 37

-Beta 2 agonist
-approved for RELAXATION OF SMOOTH MUSCLE OF UTERUS AND DELAY PREMATURE BIRTH.
-possible cardiac effects=CAUTION
-oral preffered admin.: 30% absorbed

Front 38

Dobutamine

Back 38

-Beta agonist
-synthetic analog of dopamine
-BETA 1 STIMULANT=HIGHLY SELECTIVE
-DOESNT stimulate dopamine receptors
-INCREASE CO w/o vasoconstriction
treat SHORT TERM TX OF CARDIAC INSUFFICIENCY.

Front 39

Inhibitors of reputake:

Back 39

-indirect sympathomimetics
-block NE reuptake

Front 40

Cocaine

Back 40

-reuptake inhibitor
-local anesthetic agent
-potent inhibitor of NE reuptake 1.
DRUG ABUSE

Front 41

Tricylcic antidepressent

Back 41

-reuptake inhibitor
-potent inhibitors
-used for CNS effects in treating pathological depression.