muscarinic and nicotinic blocker Flashcards
Functionally the nervous system can be divided into 3 actions which are
sensation
integration
response
autonomic efferent pathway uses how many neurons and in what arrangement to integrate the cns to peripheral organs
two neurons in series
The sympathetic dopaminergic neurons act on what organ via what receptor
renal vessels via D1 receptors
epibatidine
varenicline
lobeline
cytisine are all examples of
nicotinic agonist
choline and nicotine also(at low dose)
list 2 natural and 2 synthetic selective nicotinic agonist for ganglion(neuronal type nicotinic receptor)
natural
nicotine(small dose) and lobeline
synthetic
dimethyl phenyl piperazinium (dmpp)
tetramethyl ammonium (TMA)
ganglion stimulants are used both therapeutically and experimentally
T or F
F
they are not used therapeutically as there is no really useful purpose of stimulating both sympathetic and parasympathetic at the same time in disease state
varenicline is a partial muscarinc agonist used to assist patient in quitting smoking
T or F
F
nicotinic agonist
fill in the gaps with blockers of acetylcholine release and uptake in synapse at different stages
1.loading of ach into vessicles(VAT) - _____
2.excytosis of ach into synapse - _____
3.non-depolarizing blocking agents - _____
4.depolarizing blocking agents - _____
5.anticholinesterase - ______
6. choline transporter - ______
- Vesamicol
- botulin
- tubocurarine(can also block presynaptic ach receptors
- suxamethonium(succinylcholine)
- neostigmine
- hemicholinium
Nb: depolarizing vs non depolarizing blockers
non depolarizing blockers act competitively with acetylcholine(Competitive antagonist)
depolarizing blockers act as a ach agonist, bind to the receptor but overstimulate the post synaptic membrane leading to neuromuscular blockade and reduced sensitivity of receptors
list 4 selective m1 receptor antagonist
pirenzipine
telenzipine
dicyclomine
trihexyphenidyl
list 2 selective m2 antagonist
tripitamine
methoctramine
m3 is excitatory in nature except in what tissue of the body
vascular smooth muscle
where it elicit a vasodilatory effect via nitric oxide
on visceral smooth muscle it cause contraction
what muscarinic receptor stimulates secretion in exocrine glands and pancreas
m3 receptor
what receptor mediates the PNS effect on the eye
M3
list 4 m3 selctive antagonist
darifenacin
solifenacin
oxybutynin
tolterodine
what muscarinic receptor acts as an inhibitory auto receptor (inhibits release of ach at synapse)
M4 receptor
list 1 m4 antagonist
Himbacine
list 2 natural antimuscarinic drug
atropine
scopalamine
NOT A QUESTION
antimuscarinic drugs are divided into natural and synthetic
synthetic is divided into
1. structural analogue of atropine
2.structuraly unrelated to atropine
these 2 classifications are further divided into tertiary and quartenary amine/ammonium
ammonium for atropine analogues and amine for non atropine analogues
T
classify the antimuscarinic drug homatropine
it is a tertiary amonium synthetic structural analogue of atropine
classify homatropine methyl bromide
it is a quartenary ammonium, synthetic structural analogue of atropine
classify ipratropium and tiotropium
it is a quartenary ammonium, synthetic structural analogue of atropine
classify pirenzipine, dicyclomine and tropicamide
it is a tertiary amine , synthetic structural non related to atropine antimuscarinic drug
classify methantheline and propantheline
it is a quartenary amine , synthetic structural non related to atropine antimuscarinic drug
scopalamine is also known as
Hyoscine
4-DAMP and hexahydrosiladefenidol are examples of
M3 antagonist
atropine and scopalamine can cause the blood brain barrier
T or F
T
they are also lipid soluble
what is the effect of atropine on the heart at low doses
at low doses it causes a paradoxical bradycardia unlike at normal doses
Atropine produces excitatory effect in the CNS
T or F
T
hyoscine(scopalamine) causes sedation at low doses
T or F
T
scopalamine is also an antiemetic (used to treat motion sickness/nausea)
atropine causes temperature increase and as a mild anesthetic for the conjunctivi
T or F
F
cornea
oral and local administration of tertiary amine antimuscarinic drug is rapid absorbed while inhalation of quartenary amine drugs is minimal
T or F
T
hyoscine is better metabolized by liver and crosses the BBB better than atropine
T or F
T
atropine is only 50% metabolizable and the remaining is excreted unchanged in the urine
what is the half life of atropine
4 hrs
drugs that inhibits absorption of anticholinergic include
antacids
nb omeprazole is not an antacid
