2Nd Semester Pharmacology Acetylcholine Receptors

Front 1

what is the postganglionic neurotransmitter in the parasympathetic nervous system

Back 1

Acetylcholine (ACh)

Front 2

what is the preganglionic neurotransmitter for the sympathetic nervous system?

Back 2

Acetylcholine (ACh)

Front 3

what is the preganglionic neurotransmitter for the parasympathetic nervous system?

Back 3

Acetylcholine (ACh)

Front 4

Which ACh receptor is located in in tissues innervated by postganglionic parasympathetic neurons?

Back 4

Muscarinic

Front 5

which ACh receptor is located in presynaptic noradrenergic and cholinergic nerve terminals?

Back 5

Muscarinic

Front 6

Which ACh receptor is located in non-innervated sites in vascular endothelium?

Back 6

Muscarinic receptor

Front 7

Where are Nicotinic receptors located? 4

Back 7

· in sympathetic and parasympathetic ganglia

· in the adrenal medulla

· in the neuromuscular junction of the skeletal muscle

· in the central nervous system.

Front 8

Where are muscarinic receptors located? 4

Back 8

· in tissues innervated by postganglionic parasympathetic neurons

· in presynaptic noradrenergic and cholinergic nerve terminals

· in non-innervated sites in vascular endothelium

· in the central nervous system.

Front 9

Which ACh receptor is located in sympathetic and parasympathetic ganglia?

Back 9

Nicotinic

Front 10

Which ACh receptor is located in the adrenal medulla?

Back 10

nicotinic

Front 11

Which ACh receptor is located in the neuromuscular junction of skeletal muscle?

Back 11

Nicotinic

Front 12

What cellular change induced by binding of ACh to nicotinic receptor?

Back 12

Nicotinic receptors are ligand-gated ion channels whose activation results in a rapid increase in cellular permeability to sodium and calcium.

Front 13

Mechanism of bethanechol

Back 13

Cholinergic w/ high muscarinic (vs nicotinic) specificity.

Front 14

What are the three classes of indirect acting cholinergic drugs? how different?

Back 14

Organophosphates (very long acting)

Carbamates (long acting)

Edrophonium (short acting)

Front 15

The three ACh congeners with resistance to hydrolosis

Back 15

methacholine, carbachol, and bethanechol

Front 16

Muscarinic effect upon iris sphincter muscle

Back 16

Contraction (miosis)

Front 17

Muscarinic effect upon ciliary muscle

Back 17

Contraction (near vision)

Front 18

Muscarinic effect upon SA node

Back 18

Bradycardia

Front 19

Muscarinic effect upon AV node

Back 19

Reduced conduction velocity

Front 20

Muscarinic effect upon bronchial muscle

Back 20

Contraction

Front 21

Muscarinic effect upon Gastrointestinal motility

Back 21

Increased

Front 22

Muscarinic effect upon gastrointestinal secretion

Back 22

Increased

Front 23

Muscarinic effect uppon bladder detrusser

Back 23

Contraction

Front 24

Muscarinic effect upon bladder trigone, sphincter

Back 24

Relaxation

Front 25

Clinical uses of Bethanechol
(Urecholine®)

Back 25

improvement in gastric emptying

to treat urinary retention if physical obstruction (e.g., prostate enlargement) is not the cause.

Front 26

Pilocarpine clinical uses

Back 26

treat open-angle glaucoma (topically)

to induce salivation

Front 27

Methacholine clinical uses

Back 27

to provoke bronchoconstriction during diagnostic testing of pulmonary function (methacholine challenge )
*for the diagnosis of asthma

Front 28

methacholine mechanism

Back 28

cholinergic

Front 29

carbachol mechanism

Back 29

cholinergic

Front 30

deadly nightshade, mechanism and active ingredient

Back 30

muscarinic antagonists
atropine

Front 31

Jimson weed mechanism

Back 31

muscarinic antagonists

Front 32

Side effects of muscarinic antagonists

Back 32

constipation, xerostomia (dry mouth), hypohidrosis (decreased sweating), mydriasis (dilated pupils), urinary retention, precipitation of glaucoma, decreased lacrimation, tachycardia, and decreased respiratory secretions.

Front 33

clinical use of atropine

Back 33

raising heart rate during situations where vagal activity is pronounced (for example, vasovagal syncope).

pupil dilation

preanesthetic preparation of patients (facilitates intubation thru reduced respiratory secretions)

Front 34

inhaled ipratropium clinical use

Back 34

maintenance therapy in chronic obstructive pulmonary disease (COPD). **muscarinic antagonist, has a long half-life.

Front 35

atropine mechanism

Back 35

muscarinic antagonist

Front 36

prinzepine mechanism

Back 36

selective M1 muscarinic antagonist

Front 37

Prienzepine clinical use

Back 37

reduce gastric acid secretion (other drugs more widely used)

Front 38

the Bezold-Jarisch reflex

Back 38

bradycardia, hypotension, nausea

elicited by high doses of nicotine

Front 39

NM nicotinic receptor

Back 39

mediates skeletal muscle stimulation

Front 40

NN nicotinic receptor

Back 40

mediates stimulation of the ganglia of the autonomic nervous system

Front 41

arterioles:
Predominant System Ganglionic Blockade Effect

Back 41

Sympathetic Vasodilation

Front 42

Veins:
Predominant System Ganglionic Blockade Effect

Back 42

Sympathetic Vasodilation

Front 43

Heart:
Predominant System Ganglionic Blockade Effect

Back 43

Parasympathetic Tachycardia

Front 44

Iris:
Predominant System Ganglionic Blockade Effect

Back 44

Parasympathetic Mydriasis

Front 45

Ciliary muscle:
Predominant System Ganglionic Blockade Effect

Back 45

Parasympathetic Cycloplegia

Front 46

Gastrointestinal tract
Predominant System Ganglionic Blockade Effect

Back 46

Hypomotility

Front 47

Urinary bladder

Back 47

Predominant System Ganglionic Blockade Effect

Front 48

Salivary glands
Predominant System Ganglionic Blockade Effect

Back 48

Parasympathetic Xerostomia

Front 49

Sweat glands Predominant System Ganglionic Blockade Effect

Back 49

Sympathetic cholinergic Anhidrosis

Front 50

"Reversible" cholinesterase inhibitors. 1 which enters CNS, 2 which do not

Back 50

physostigmine that enters the CNS

neostigmine and edrophonium that do not

Front 51

Neostigmine clinical use

Back 51

stimulate motor activity of the small intestine and colon

treating atony of the detrusor muscle of the urinary bladder

myasthenia gravis

glaucoma, sometimes

Front 52

Neostigme mechanism

Back 52

"reversible" cholinesterase inhibitor which does not enter CNS

Front 53

Edrophonium clinical use

Back 53

"tensilon test' of myasthenia gravis

Front 54

side effects of physostigmine, 4

treatment

Back 54

nausea, pallor, sweating and bradycardia

anticholinergic drugs which are quaternary amines do not enter CNS

Front 55

drug for treatment of anticholinergic syndrome

Back 55

Physostigmine

Front 56

new cholinesterase inhibitors for treating alzheimers

Back 56

(Aricept®) and rivastigmine (Exelon®) have little hepatotoxicity and have replaced tacrine

Front 57

drug to counteract intoxication by cholinesterase inhibitor

Back 57

pralidoxime

Front 58

Clinical Manifestations of Cholinesterase Inhibitor Intoxication: Muscarinic
13

Back 58

· Miosis

· Blurred vision (spasm of accommodation)

· Lacrimation

· Sweating

· Excessive respiratory secretions

· Dyspnea (bronchoconstriction)

· Bradycardia

· Hypotension

· Salivation

· Nausea

· Cramping (gastrointestinal spasm)

· Diarrhea

· Urgency (urinary incontinence)

Front 59

Clinical Manifestations of Cholinesterase Inhibitor Intoxication: Nicotinic

3

Back 59

· Fasciculations (early)

· Weakness (late)

· Adrenomedullary (sympathetic) discharge (early and transient)

Front 60

Clinical Manifestations of Cholinesterase Inhibitor Intoxication: CNS
9

Back 60

· Anxiety

· Insomnia

· Nightmares

· Confusion

· Hypertension (rare)

· Tremors

· Convulsions

· Respiratory depression

· Circulatory collapse

Front 61

Therapy of Cholinesterase Inhibitor Intoxication, mild poisoning
4

Back 61

· Atropine sulfate, 1-2 mg intravenously, as necessary

· Termination of exposure

· Pralidoxime, 1 g infused slowly, or 1-3 orally (if no GI symptoms)

· Supportive care

Front 62

Therapy of Cholinesterase Inhibitor Intoxication
severe poisoning, 7

Back 62

· Artificial respiration

· Atropine sulfate, 2-4 mg intravenously at 5 minute intervals until abatement of symptoms occurs or signs of atropinization (tachycardia, dilated pupil, drug skin) appear

· Pralidoxime, 1 g infused slowly

· Termination of exposure

· If convulsion, diazepam 5-10 mg intravenously

· Supportive care

· Hospitalization for 2-3 days

Front 63

effect of cholinesterase inhibitor on depolarizing vs nondepolarizing neuromuscular blocking druges

Back 63

can overcome non depolarizing

Front 64

Tubocuranine mechanism

Back 64

Nondepolarizing neuromuscular blocking

Front 65

Succinylcholine mechanism

Back 65

Depolarizing neuromuscular blocking

Front 66

order of muscel parayzation by muscle blocker

Back 66

extraocular muscles are affected first, then the muscles of the hands and feet, head and neck, abdomen and limbs, and finally the muscles of ventilation

Front 67

Dantrolene mechanism

Back 67

reduces the release of activator calcium from the sarcoplasmic reticulum

Front 68

dantrolene clinical use

Back 68

treat the muscle contractures associated with malignant hyperthermia

*not usefull for acute muscle spasm

Front 69

Baclofen mechanism

Back 69

partial GABA agonist, probably in the spinal cord.

muscle relaxant

Front 70

strychnine mechanism

Back 70

enhances glycine inhibitory effects