Pharm 1 - Cholinergic Antagonists (Smith)

Front 1

Atropine and scopolamine

Back 1

Can block all 5 muscarinic receptors

Front 2

M1 receptor

Back 2

Linked to phopholipase C - Found in nerves and CNS

Front 3

M2 receptor

Back 3

Inhibitory with adenyl cyclase (less cAMP and increase efflux of K+)
Found in stomach and heart

Front 4

M3 receptor

Back 4

Linked to phospholipase C
Found in glands

Front 5

M5 receptor

Back 5

Linked to phospholipase C
Nerves and CNS

Front 6

M4 receptor

Back 6

Inhibitory with adenyl cyclase (less cAMP and increase efflux of K+)
Nerves and CNS

Front 7

Dycyclomine

Back 7

Antispasmodic and anti-irritable bowel syndrome (causes constipation).

Front 8

Trihexylphenidyl or benztropine

Back 8

Parkinson's

Front 9

Gallamine

Back 9

MNJ blocker

Front 10

Nicotinic receptors

Back 10

Found in ganglia and MNJ
Na+/K+ ion channels.

Front 11

Atropine

Back 11

Muscarinic blocker
Intensifies symp effects on an organ

Mad as a hatter - delirium
Blind as a bat - mydriasis, photophobia, blurred vision
Dry as a bone - dry mouth and less sweating
Red as a beet - Fever, anhidrosis
Hot as a hare - Anhidrosis
Urinary retention, bronchodilation, constipation, tachycardia.

Front 12

Scopolamine

Back 12

Induce amnesia or to tx motion sickness.

Front 13

Iprtropium or tiotropium

Back 13

Asthma

Front 14

Constipation

Back 14

Dicyclomine

Front 15

Perenzipine

Back 15

Managing peptic ulcers

Front 16

Succinylcholine

Back 16

The only DEPOLARIZING blocker at MNJ

Two molecules of ACh joined. Works at MNJ and not the ganglia.

Given as IV. Cleared by plasma ChE - pts lacking this are paralyzed for hours.

large muscles (chest, abdomen) affected first (flaccidity)

Histamine release to produce vasodil and warmth

Malignany hyperthermia rarely from release of Ca++ from sarcoplasmic reticulum

Rigid muscles, acidosis, high fever

ANES gases and aminoglycoside antibiotics synergize with succinylcholine.

Front 17

Mechanism of how ACh and nicotine can block nicotinic receptors

Back 17

After muscle fasciculations, there is persistent occupation and prolonged depolarization where the receptor doesn't respond to any stimulus (phase 1 block)

Phase 2 block - Receptor is dessens to agonists but will respond to other stimuli (depolarization-desensitization block)

Can't terminate this block.

Front 18

How to tx succinylcholine fever, rigid muscles and acidosis

Back 18

Ice bath, bicarb and dantrolene

Front 19

Curare

Back 19

Nondepol MNJ blocker.

Causes paralysis with intact sensorium.

Front 20

Neostigmine contraindicated with...

Back 20

succinylcholine paralysis.

Front 21

Pancuronium

Back 21

Nondepol MNJ blocker
Cleared renally

Front 22

vercuronium

Back 22

Nondepol MNJ blocker
Cleared by liver

Front 23

Rocuronium

Back 23

Nondepol MNJ blocker
Cleared by liver

Front 24

Cisatracurium

Back 24

Nondepol MNJ blocker
Cleared by liver/plasma esterases.

Front 25

General char about nondepol MNJ blockers

Back 25

Pancuronium, rocuronium, vercuronium, cisatracurium

Small muscles affected before large (contrast with succinylcholine)
Reverse with neostigmine
SEs are tachycardia, HTN, hsitamine release, interactions with inhaled anesthetics and aminoglycosides

Front 26

Ganglion blocker

Back 26

Trimethaphan blocks all ganglia, but used for its anti-sympathetic effects

Tx of HTN crisis and teh effects last for minutes (cleared by liver)

SE - orthostatis HTN, urinary retention, constipation, impaired accom of lens fo eye (this is a parasymp blockade at the ganglionic level)

Front 27

Botulinum toxins

Back 27

Block release of ACh
Interferes with docking proteins on interior of the nerve membrane.
Leads to flaccid paralysis
Produces signs of atropine poisoning without CNS effects

BoTox - remove facial wrinkles and prevent hyperhydrosis.