Glossary of med chem cholinergic antagonists
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- cholinergic antagonist
- drug that interfers with ACh at cholinergic receptors
- a compound that has an affinity for the receptor but lacks intrinsic activity
binds but will not produce a response
- 2 types of nicotinic antagonists
- ganglionic blockers
neuromuscular blocking agents
- muscarinic antagonists aka (7)
*parasympathetic postganglionic blocking agent
- muscarinic antagonist clinical manifestations: heart
- muscarinic antagonist clinical manifestations: lungs
- dilation of bronchioles
- muscarinic antagonist clinical manifestations: GI tract
- decr secretion & motility
- muscarinic antagonist clinical manifestations: bladder
- urinary retention
- muscarinic antagonist clinical manifestations: eyes
- pupil dilation
- temporary paralysis of ciliary muscle
- muscarinic antagonist clinical manifestations: skeletal muscle
- muscarinic antagonist clinical manifestations: CNS
- CNS stimulation or depression
- muscarinic antagonist clinical manifestations: mucous membrane
- decr salivation and perspiration
- clinical significance of antimuscarinics (uses, effects)
- incr cardiac output
mydriatic & cycloplegia
- how can an antimuscarinic treat bradyarrythmia?
- incr heart rate
- what significance does the antispasmodic effect of antimusc have?
- used to treat diahrrea - tone & motility of GIT
- what significance does the antisecretory effect of antimusc have?
- can be used prior to surgery
antisialoqoque (prevent drooling)
antihydrotic (prevent excessive perspiration)
- why can an antimuscarinic be used to treat asthma or COPD
- b/c antimusc cause bronchodilation
- what are the most common side effects of antimuscarinics?
- dry mouth
- how do antimusc precipitate glaucoma?
- pupils dilate -> ciliary muscle thickens -> anterior chamber narrows -> obstruct outflow of aq humor -> incr intraocular pressure
- what are the 6 classes of antimuscarinics
- solanaceous alkaloids
- give 2 examples of solanaceous alkaloids
- atropine is derived from what plants?
- atropa belladona (deadly nightshade)
datura stramonium (jimsonweed, thorn apple)
- what plant is scopolamine derived from?
- hyoscymus niger (black henbane)
- another name for atropine
- what bicyclic ring does atropine contain? what 2 rings make up the bicyclic ring?
- what position must the 3 alpha hydroxy group be in for atropine to be active?
- axial position
- neurotropic effect
- interfering with nerve impulse transmission
- musculotropic effect
- direct depression of smooth muscle, esp of the GIT
standard - papavarine
- atropine sulfate is used primarily for?
- mydriatic effect during eye exams/refraction studies
- other effects of atropine sulfate?
decr GIT secretions
- atropine sulfate is contraindicated in patients with:
- open angle glaucoma
- scopolamine is AKA
- can scopolamine penetrate the CNS?
- yes b/c it has no charge
- what important group is found in scopolamine
- beta-epoxy group
- what is scopolamine used for?
- to prevent motion of sickness - drug of choice
- what are side effects of scopolamine?
- homatropine HBr is similar to what other drug?
- homatropine HBr is an ester of what 2 acids
- tropine acid
- what is the potency of homatropine compared to atropine?
- 1/2 as potent as atropine
- homatropine is used primarily for what properties?
- mydriatic and cycloplegic proterties
- what is the brand name for ipratropium br?
- how is ipratropium related to atropine?
- it is a semi-synthetic derivative of atropine
- what is the mechanism of action of ipratropium bromide
- produces bronchodilation by competitive inhibition of cholinergic receptors bound to smooth muscles of bronchioles
- ipratroium br is used to treat:
- asthma (as an adjuvant) & COPD
- list of 9 drugs that are aminoalcohol esters
- clidinium br
- brand name for clidinium bromide
- clidinium bromide contains what kind of nucleus?
- clidinium bromide is used for which effects?
- its antispasmodic & antisecretory effects
- clidinium br is used in combination with chlordiazepoxide to treat
- peptic ulcers & other GI secretory diseases
- brand name for clidinium br & chlordiazepoxide combo
- librax has more affinity for which receptors?
- M1 & M3 (CNS & GIT)
- brand name for dicyclomine hcl
- activity of dicylomine as it relates to atropine (neurotropic & musculotropic)
- 1/8 neurotropic activity & 2x musculotropic activity as atropine
- dicyclomine used primarily for its
- spasmolytic effet on smooth muscle of GIT; IBS
- can dicylomine penetrate the CNS?
- yes - no charge
- brand name for glycopyrrolate
- can glycopyrrolate penetrate the CNS?
- no - quaternary ammonium
- what kind of ring does glycopyrrolate have?
- pyrrolidine ring
- glycopyrrolate used for:
- spasmolytic & antisecretory effect
- glycopyrrolate has more affinity for which receptor?
- M1 (less tachycardia as side effect)
- what occurs as a result of high doses of glycopyrrolate
- NMJ and ganglionic receptors can be blocked
- brand name for propantheline br
- propantheline br is a derivative of what drug?
- banthine (methantheline)
-ethyl instead of isopropyl groups
-2-5x more potent
- what ring does propantheline br have?
- xanthene ring
- propantheline br is used for
- antispasmodic & antisecretory effects
- aminoalcohol esters are mostly used for
- antispasmodic & antisecretory effects
- aminoalcohol esters - quaternary ammonium derivatives
- poorly absorbed
little or no CNS effect
can block ganglionic and NMJ receptors in high doses
- aminoalcohol ethers and aminoalcohols are used to
- manage symptoms of PD
- examples of aminoalcohol ethers
- benztropine mesylate
- examples of aminoalcohols
- Parkinson's disease first described by who? in what year?
- james parkinson
- parkinson's disease aka
- shaking palsey
- 4 primary symptoms of PD
- fine tremors (pill rolling)
rigidity or stiffness of limbs, trunk
slowness of movement (bradykinesia)
- other symptoms of PD
- oculogyric crisis
- oculogyric crisis
- movement of eyeballs impaired - positioned upward & outward
- where does PD orginate
- in the midbrain
- what does the substantia nigra produce?
- what is the substantia nigra
- deeply pigmented grey cells
- pyrimidal tract
initiates muscle movement
- extrapyrimidal tract
smooths and coordinates muscle movement
- what kind of neurotransmittor is dopamine?
- in healthy individuals, dopamine relays signals from the substantia nigra to the next relay station, the:
- corpus stiatum
- what produces purposeful muscle activity
- balance of inhibitory dopamine (extrapyrimidal) & excitatory ACh (pyrimidal) mediated neurotransmission
- pathophysiology of PD
- the dopamine producing neurons in the substantia nigra die
imbalance between dopaminergic & cholinergic activity leaves the patient unable to control movement in a normal manner
- primary PD is AKA
- paralysis agitans
- is the cause of primary PD known?
- no (idiopathic)
- is primary PD curable?
- no - treatment is palliative
- what are the causes of secondary PD?
- drugs (iatrogenic - reversible)
- drugs that induce secondary PD
- infectious causes of secondary PD
- other causes of secondary PD
- objective of PD treatment
- to improve quality of life
- what are the 2 types of drugs used to treat PD
- dopaminergic agonists
cholinergic antagonists (for mild symptoms - tremors)
- brand name for diphenhydramine
- what effect does diphenhydramine have?
some anticholinergic activity
alleviates some symptoms of PD
- brand name for benztropine mesylate
- what 3 effects does benztropine have?
- benzotropine has similar potency and side effects as what drug?
- benztropine should not be used in patients with:
- benign prostratic hyperplasia
- the prostate is enlarged, which pinches the urethra causing painful urination
- what are the common structural features of aminoalcohols
- bulky groups in the vicinity of hydroxyl and cyclic amino functional groups
- tertiary amines used to treat:
quaternary amines used for:
- what is the brand name for biperiden
- what ring structure does biperiden have?
- piperidine ring
- biperiden is used to treat
- all forms of PD
spastic disorders (spinal cord injury, cerebral palsey, multiple schlerosis)
akinesia, rigidity, tremor
- brand name for procyclidine HCl
- characteristics of procyclidine
- pyrrolidine ring
tertiary amine - PD
- brand name for trihexyphenidyl HCl
- chracteristics of trihexyphenidyl
- piperidine ring
used in PD
1/2 as potent as atropine
good margin of safety
- brand name for isopropamide iodide
- isopropamide used to treat?
- peptic ulcers
- DOA of isopropamide
- 12 hrs
- isopropamide is contraindicated for patients with:
- brand name for ethopropazine HCl
- ring in ethopropazine
- ethopropazine used to treat:
- PD (controls rigidity, tremors, sialorrhea, oculogyric crises)
- side effects of ethopropazine?
- papaverine is a derivative of what plant?
- papaver somniferum
- papaverine has what kind of structure
- MOA of papaverine
- generalized smooth muscle relaxation
- papaverine used to treat
- peripheral vascular diseases (spasmolytic activity)
- papaverine not used often b/c?
- lack of potency
- what is raynaud's disease
- vascular disease
cyanosis of fingers, nails b/c of impaired blood flow
- what are the 2 types of nicotinic antagonists
- ganglionic blocking agents
neuromuscular blocking agents
- what are the 3 kinds of ganglionic blocking agents?
- what are the 2 kinds of neuromuscular blocking agents?
- what was the 1st class of drugs used for hypotensive effect?
- neuromuscular blockers
- a drug that blocks the sympathetic system is known as:
- a drug that blocks the parasympathetic system is known as:
- what affects do sympathoplegia drugs have?
- orthostatic hypotension
- what affects do parasympathoplegia drugs have?
precipitation of glaucoma
- in what NS do ganglionic blockers work? neuromuscular blockers?
- what stimulant is a depolarizing ganglionic blocking agent?
- at low doses, nicotine is a _______; at high doses, it is a ________
- stimulant (depol & repol)
ganglionic blocker (no repolarization)
- what therapeutically useful drugs are there in the depolarizing gangionlic blockers group?
- MOA of nondepolarizing comkpetitive ganglionic blocking agents
- bind to nicotinic receptor but lack intrinsic activity for impulse transmission (unable to depolarize the cell)
- name 5 examples of nondepolarizing competitive ganglionic blocking agents
- tetramethylammonium salts
- what is the difference between hexamethonium and decamethonium
- hexa: 6c, strong ganglionic blocker, weak curariform activity
deca: 10c, weak gang blocker, strong curariform activity
- brand name for trimethaphan camsylate
- what ring structure does trimethaphan camselate have?
- camphor sulfonate
- DOA of trimethaphan
- short, 10-30 min
- use for trimethaphan
- used in emergency room to lower BP (given by iv, inactive orally)
- brand name for mecamylamine
- what ring structure does mecamylamine have?
- norbornane ring
- what is mecamylamine rarely used?
- causes severe orthostatic hypotension
- curariform activity AKA
- neuromuscular blocking activity
- what is a NMJ?
- specialized synapse between a motor neuron and skeletal muscle
- when are neuromuscular blocking agents commonly used?
- during surgical procedures as adjuncts to general anesthesia
- what are NM blocking agents used during surgery?
- induce reversible paralysis
no central activity
- what is the prototype for nondepolarizing NMJ blockers?
- example of a depolarizing NMJ blocker
- tubocurarine is derived from what plant?
- curare (chondodendron tomentosum)
- what is the half life of tubocurarine?
- 90 min
- DOA of tubocurarine
- 2 hrs (binds at receptor for only 1 msec)
- uses for tubocurarine
- adjunct in general anesthesia
- the brand name for atracurium besylate
- DOA of atracurium?
- short - 20min b/c easily hydrolyzed by plasma esterases
- what 2 ring structures does atracurium have?
- which is more potent: atracurium or tobocurarine?
- atracurium, 2.5x
- uses for atracurium?
- skeletal muscle relaxant for short surgical procedures
- paralysis caused by atracurium can be reversed by? how?
- AChEI - incr amount of ACh present, competes with drug for receptor
- why can atracurium be dangerous if you are on it for a long time?
- metabolyte can accumulate in the brain & cause seizures
- what is laudanosine?
- breakdown product of atracurium
- what is the brand name for doxacurium cl?
- what ring complex does doxacurium have?
- what is the difference between atracurium & doxacurium?
- doxa has an extra methoxy group - hinds access of esterases - longer doa
- uses for doxacurium
- skeletal muscle relaxant for surgical procedures lasting longer than 90 min
- what is the brand name for pancuronium bromide?
- what ring complex does pancuronium have?
- amino steroid
- what 2 placess does pancuronium act?
- nicotinic receptor
- which is more potent: tubocurarine or pancuronium?
- pancuronium, 5x
- uses for pancuronium
- skeletal muscle relaxant during surgery
adjunct to anesthesia
- what are the possible metabolytes of pancuronium?
- brand name for succinyl cl
- what class does succinly cl belong to?
- depol NMJ blocker - only useful agent in its class
- doa of succinyl cl?
- very short acting
- succinyl cl is unstable in what kind of soln?
- uses for succinyl cl
- skeletal muscle relaxant in surgery
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