Drugs Cholinomimetics/and cholinergic receptors

Question 1

Another name for cholinomimetics

Answer 1

parasympathomimetics

Question 2

Direct Cholinomimetics name them and what is direct

Answer 2

Direct=mimic activity of acetylcholine by directly binding to muscarinic and nicotinic receptors as agonist

Acetylcholine
Methacholine
Carbachol
Bethanechol

Muscarinic

Nicotinic

Question 3

Muscarinic drugs

Answer 3

Muscarine
Pilocarpine

Question 4

Nicotinic drugs

Answer 4

Nicotine
Arecoline

Question 5

Indirect Cholinomimetics name and how they work

Answer 5

Indirect=block acetylcholinesterase to increase Ach in synapse leading to more Ach binding

Edrophonium
Neostigmine, pyridostigmine
Echothiophate

Question 6

parasympathomimetics are useful in treating conditions like (name 3)

Answer 6

1) glaucoma
2) myanthenia gravis
3) alzheimer’s

Question 7

parasympathomimetic drugs work by

Answer 7

enhancing the activity of the parasympathetic nervous system by 1) directly stimulating the cholinergic receptors or 2) indirectly increased Ach levels

Question 8

how to parasympatholegic drugs work

Answer 8

drugs that inhibit the PNS by blocking Ach from binding to its site

primarily block it from muscarinic receptors

Question 9

name the cholinergic excitatory receptors

Answer 9

M1, M3, M5

Question 10

name the cholinergic inhibitory receptors

Answer 10

M2, M4

Question 11

PNS nicotinic receptor found in the ganglion

Answer 11

nicotinicN(neuronal)

Question 12

PNS nicotinic receptor found at the skeletal muscle end plates

Answer 12

nicotinicM(muscular)

Question 13

cholinergic nicotinic receptors are found in the

Answer 13

ganglionic, skeletal muscle(ion channels not GPCR’s) and neuronal CNS

Question 14

muscarinic cholinergic receptors found in the

Answer 14

heart, lungs, and smooth muscle

Question 15

cholinergic receptors respond to

Answer 15

Ach to act on the PNS

Question 16

generic PNS in the heart

Answer 16

HR and contractility decrease when Ach binds to M2

Question 17

generic PNS in the smooth muscle blood vessels

Answer 17

vasodilate when Ach binds to M3

Question 18

generic PNS in the bronchiole smooth muscle

Answer 18

bronchoconstricts when Ach binds to M3

this is bad for asthma ppl

Question 19

Name 4 major clinical uses for cholinomimetic agonists

Answer 19

1) mimic Ach effects
2) direct acting by binding directly to muscarinic or nicotinic receptors to stimulate Ach effects
3) when binding to nicotinic receptors it causes neuromuscular end plate depolarization and skeletal contraction
4) when binding to muscarinic receptors causes slow down HR

Question 20

what kind of receptor is nicotinic and what is effect

Answer 20

ion channel receptor

when binding to nicotinic receptors it causes neuromuscular end plate

agonist–> muscle contractions, shakiness, tremors

antagonist–> paralyzes skeletal muscle

Question 21

what kind of receptor is muscarinic

Answer 21

GPCR

agonist–> slows down HR
antagonist–> speeds up HR

when binding to muscarinic receptors causes slow down HR

Question 22

what cholinergic agonist has a effect on the eye and what is that effect

Answer 22

muscarinic agonist causes contraction of the pupil

increases intraocular drainage

Question 23

cardiac effect from cholinergic agonist

Answer 23

reduction in peripheral vascular resistance

vasodilation–> HR picks up due to reduced BP

Question 24

cholinergic effect on respiratory system

Answer 24

smooth muscle of the bronchial tree constrict so better airway tone

mucosa secretion increased

all bad for asthma bc increased secretions and dilation means dust comes in

Question 25

cholinergic agonist effect on GI

Answer 25

increased secretory/motility

salivary and gastric glands stimulated

sphincters relax

Question 26

cholinergic agonist effect on brain

Answer 26

muscarinic mostly

nicotinic sites for smoking–> large doses give you tremors, emesis, convulsions, coma

Question 27

cholinergic agonist effects on spinal cord

Answer 27

mostly nicotinic sites

Question 28

neuromuscular junction (NMJ) and cholinergic receptors

Answer 28

nicotinicM(muscular) receptors cause end plate depolarization so muscle contraction bc of increased Na and K permeability

Question 29

what is glaucoma and how do cholinomimetics help it

Answer 29

Glaucoma is excess amount of intraocular fluid (aqueous humor) formed by ciliary epithelium and drains into canal of schlemm

intraocular drains bc of a flat iris and wide angles so if too much fluid then can give methacholine or bethanechol(cholinomimetics) to constrict the pupil which flattens iris even more

Question 31

difference between nicotinic neuronal and nicotinic muscular receptors

Answer 31

NN–> found in the CNS so both SNS and CNS; involved in communication btw post and preganglionic neurons
-have beta and alpha receptors
-THINK NEURAL SIGNALING WITH ANS AND CNS

NM–> located in the NMJ of skeletal muscle so communication btw neurons and muscle fibers
-Ach binding to these leads to muscle contraction
-THINK SKELETAL MUSCLE CONTRACTION

Question 32

what are the acute nicotine toxicity signs

Answer 32

headaches, nausea, dizziness, breathlessness, collapsing

little bit different from muscarinic toxicity

Question 33

what do you do for acute nicotinic toxicity

Answer 33

usually from ingesting cigarettes

induce vomiting

Question 34

s/s of organophosphate insecticide poisoning

Question 35

how does acetylcholinesterase work

Question 36

describe organophosphate aging

Answer 36

in muscarinic toxicity

when organophosphate binds to acetylcholinesterase it starts to age and the rate of aging depends on organophosphate–> can take time but the longer it binds the stronger the bond gets and the harder it is to strip the organophosphate off from the receptor site bc of the covalent bond

Question 37

s/s of muscarinic toxicity(organophosphate poisoning)