Pharma Topic List B Flashcards
B.3. Cholinomimetics - Drugs
carbachol
pilocarpine
neostigmine
pyridostigmine
rivastigmine
edrophonium
B.3. Cholinomimetics - Effects
i.e. parasympathomimetics – Rest and Digest
Eye - contraction of iris sphincter and ciliary m.
Salivary - inc secretion
Heart - inc vagal - negative chronotropy, dromotropy, inotropy
BV - dec BP - smooth muscle relaxation
Lungs - Bronchoconstriction
Stomach - inc gastric secretion
Intestine - inc motility
Urinary Tract - alleviate retention
B.3 Cholinmemtics - AChEi poisoning
DUMBBELS
D - diarrhea
U - urination
M - miosis
B - bradycardia
B - bronchoconstriction
E - excitation - CNS, muscles
L - lacrimation
S - secretion - sweating, salivation
carbachol
Is a synthetic choline ester
Direct acting cholinomemtic that is highly resistant to AchE hydrolysis
Acts on both N and M - not specific so rarely used
4˚ amine - no BBB
Topical - eyedrops
t1/2= 1 hr
tx: Acute Angle Glaucoma - opens canal of Schlemm
SE - CV and GI effect - stimulates and then depresses
N-R can cause release of E from adrenal medulla
B.3. Cholinomimetics
pilocarpine
Direct acting Cholinomimetic - Alkaloid so it is specific for muscarinic - Muscarinic Agonist
3˚ amine Yes BBB
Resistance to AchE hydrolysis
PO (eyedrops), Parentral
DoA - 30 min - 2h
Tx - Xerostoma from Sjøgren - systemic
DoC - glaucoma
OD- Antidote Atropine
B.3. Cholinomimetics
neostigmine
Indirect Acting Cholinomimetic
Non-competitive AchEi
4˚amine - no BBB
its a carbamate
main site of action is NMJ
IV - poor absorption in GI
tx: non-obstructive ileus, urinary retention
Used as an antidote for non-depolarizing curare like drugs post-op
CI - intestinal or urinary obstruction
B.3. Cholinomimetics
pyridostigmine
Indirect acting - Non-competitive AchEi
4˚amine - NO BBB
PO
DoA = 3-6hr
Main site of action - NMJ
tx: DoC for Myasthenia Gravis
paralytic ileus, urinary bladder atony
can be used against nerve gases
B.3. Cholinomimetics
rivastigmine
Non-Competitive AchEi - Indirect acting Cholinomemtic
Long acting t1/2 = ±70 hr
lipid soluble - YES BBB
hydrolyzed to carbamylated metabolite - no interactions
tx: transdermal patch - Alzheimer’s
first line drug with Donepezil, Galantamine
can delay the progession but cannot stop the disease
SE - GI distresss, cholinergic sym subside with continuing use
B.3. Cholinomimetics
edrophonium
Competitive AchEi
Short acting t1/2 = 5-15 mins with rapid renal elimination
to short for therapeutic use
PO
4˚amine - limited to periphery
Used: Tensilon test for diagnosis of Myasthenia Gravis
If too much given - antidote with atropine
B.3. Cholinomimetics
B.4. Muscarinic receptor blocking drugs
atropine
scopolamine
butyl-scopolamine
ipratropium
procyclidine
solifenacin
cyclopentolate
tiotropium
oxybutinine
atropine
B.4. Muscarinic receptor blocking drugs
scopolamine
B.4. Muscarinic receptor blocking drugs
butyl-scopolamine
B.4. Muscarinic receptor blocking drugs
ipratropium
B.4. Muscarinic receptor blocking drugs
procyclidine
B.4. Muscarinic receptor blocking drugs
solifenacin
B.4. Muscarinic receptor blocking drugs
cyclopentolate
B.4. Muscarinic receptor blocking drugs
tiotropium
B.4. Muscarinic receptor blocking drugs
oxybutinine
B.4. Muscarinic receptor blocking drugs
B.5. Catecholamines - Drugs
epinephrine
norepinephrine
dopamine
isoprenalin
dobutamine
epinephrine
B.5. Catecholamines
norepinephrine
B.5. Catecholamines
dopamine
B.5. Catecholamines
isoprenalin
B.5. Catecholamines