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180 Cards in this Set
- Front
- Back
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cholinergic antagonist
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drug that interfers with ACh at cholinergic receptors
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antagonist
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a compound that has an affinity for the receptor but lacks intrinsic activity
binds but will not produce a response |
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2 types of nicotinic antagonists
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ganglionic blockers
neuromuscular blocking agents |
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muscarinic antagonists aka (7)
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antimuscarinic
anticholinergic cholinergic antagonist cholinergic blocker parasympatholytics *parasympathetic postganglionic blocking agent antispasmodic |
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muscarinic antagonist clinical manifestations: heart
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tachycardia
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muscarinic antagonist clinical manifestations: lungs
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dilation of bronchioles
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muscarinic antagonist clinical manifestations: GI tract
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decr secretion & motility
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muscarinic antagonist clinical manifestations: bladder
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urinary retention
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muscarinic antagonist clinical manifestations: eyes
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mydriasis
cycloplegia |
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mydriasis
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pupil dilation
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cycloplegia
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temporary paralysis of ciliary muscle
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muscarinic antagonist clinical manifestations: skeletal muscle
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relaxation
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muscarinic antagonist clinical manifestations: CNS
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CNS stimulation or depression
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muscarinic antagonist clinical manifestations: mucous membrane
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decr salivation and perspiration
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clinical significance of antimuscarinics (uses, effects)
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incr cardiac output
antispasmodic effect antisecretory effect mydriatic & cycloplegia PD asthma cholinergic poisoning |
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how can an antimuscarinic treat bradyarrythmia?
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incr heart rate
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what significance does the antispasmodic effect of antimusc have?
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used to treat diahrrea - tone & motility of GIT
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what significance does the antisecretory effect of antimusc have?
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can be used prior to surgery
antisialoqoque (prevent drooling) antihydrotic (prevent excessive perspiration) |
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why can an antimuscarinic be used to treat asthma or COPD
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b/c antimusc cause bronchodilation
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what are the most common side effects of antimuscarinics?
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dry mouth
mydriasis urinary retention precipitate glaucoma |
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how do antimusc precipitate glaucoma?
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pupils dilate -> ciliary muscle thickens -> anterior chamber narrows -> obstruct outflow of aq humor -> incr intraocular pressure
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what are the 6 classes of antimuscarinics
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solanaceous alkaloids
aminoalcohol esters aminoalcohol ethers amino alcohols aminoamides miscelleneous |
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give 2 examples of solanaceous alkaloids
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atropine
scopolamine |
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atropine is derived from what plants?
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atropa belladona (deadly nightshade)
datura stramonium (jimsonweed, thorn apple) |
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what plant is scopolamine derived from?
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hyoscymus niger (black henbane)
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another name for atropine
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hyoscyamine
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what bicyclic ring does atropine contain? what 2 rings make up the bicyclic ring?
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tropane
piperidine n-methyl pyrrolidine |
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what position must the 3 alpha hydroxy group be in for atropine to be active?
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axial position
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neurotropic effect
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interfering with nerve impulse transmission
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musculotropic effect
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direct depression of smooth muscle, esp of the GIT
standard - papavarine |
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atropine sulfate is used primarily for?
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mydriatic effect during eye exams/refraction studies
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other effects of atropine sulfate?
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tachycardia
constipation xerostomia dry eyes CNS stimulation decr GIT secretions |
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atropine sulfate is contraindicated in patients with:
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open angle glaucoma
BPH severe hypertension |
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scopolamine is AKA
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hyoscine
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can scopolamine penetrate the CNS?
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yes b/c it has no charge
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what important group is found in scopolamine
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beta-epoxy group
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what is scopolamine used for?
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to prevent motion of sickness - drug of choice
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what are side effects of scopolamine?
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sedation
dry mouth |
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homatropine HBr is similar to what other drug?
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atropine
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homatropine HBr is an ester of what 2 acids
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tropine acid
mandelic acid |
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what is the potency of homatropine compared to atropine?
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1/2 as potent as atropine
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homatropine is used primarily for what properties?
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mydriatic and cycloplegic proterties
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what is the brand name for ipratropium br?
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atrovent
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how is ipratropium related to atropine?
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it is a semi-synthetic derivative of atropine
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what is the mechanism of action of ipratropium bromide
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produces bronchodilation by competitive inhibition of cholinergic receptors bound to smooth muscles of bronchioles
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ipratroium br is used to treat:
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asthma (as an adjuvant) & COPD
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list of 9 drugs that are aminoalcohol esters
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clidinium br
cyclopentolate HCl dicyclomine HCl eucatropine HCl glycopyrrolate mepenzolate br methantheline br oxyphencyclamine hcl propantheline br |
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brand name for clidinium bromide
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quarzan
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clidinium bromide contains what kind of nucleus?
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quinuclidine
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clidinium bromide is used for which effects?
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its antispasmodic & antisecretory effects
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clidinium br is used in combination with chlordiazepoxide to treat
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peptic ulcers & other GI secretory diseases
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brand name for clidinium br & chlordiazepoxide combo
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librax
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librax has more affinity for which receptors?
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M1 & M3 (CNS & GIT)
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brand name for dicyclomine hcl
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bentyl
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activity of dicylomine as it relates to atropine (neurotropic & musculotropic)
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1/8 neurotropic activity & 2x musculotropic activity as atropine
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dicyclomine used primarily for its
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spasmolytic effet on smooth muscle of GIT; IBS
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can dicylomine penetrate the CNS?
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yes - no charge
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brand name for glycopyrrolate
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robinul
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can glycopyrrolate penetrate the CNS?
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no - quaternary ammonium
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what kind of ring does glycopyrrolate have?
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pyrrolidine ring
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glycopyrrolate used for:
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spasmolytic & antisecretory effect
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glycopyrrolate has more affinity for which receptor?
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M1 (less tachycardia as side effect)
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what occurs as a result of high doses of glycopyrrolate
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NMJ and ganglionic receptors can be blocked
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brand name for propantheline br
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pro-banthine
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propantheline br is a derivative of what drug?
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banthine (methantheline)
-ethyl instead of isopropyl groups -2-5x more potent |
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what ring does propantheline br have?
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xanthene ring
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propantheline br is used for
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antispasmodic & antisecretory effects
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aminoalcohol esters are mostly used for
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antispasmodic & antisecretory effects
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aminoalcohol esters - quaternary ammonium derivatives
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poorly absorbed
little or no CNS effect can block ganglionic and NMJ receptors in high doses |
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aminoalcohol ethers and aminoalcohols are used to
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manage symptoms of PD
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examples of aminoalcohol ethers
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benztropine mesylate
orphenadrine citrate |
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examples of aminoalcohols
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biperidine
procyclidine trihexyphenidyl HCl |
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Parkinson's disease first described by who? in what year?
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james parkinson
1817 |
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parkinson's disease aka
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shaking palsey
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4 primary symptoms of PD
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fine tremors (pill rolling)
rigidity or stiffness of limbs, trunk slowness of movement (bradykinesia) postural instability |
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other symptoms of PD
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oculogyric crisis
mask face drooling depression |
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oculogyric crisis
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movement of eyeballs impaired - positioned upward & outward
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where does PD orginate
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in the midbrain
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what does the substantia nigra produce?
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dopamine
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what is the substantia nigra
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deeply pigmented grey cells
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pyrimidal tract
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excitatory
initiates muscle movement |
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extrapyrimidal tract
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inhibitory
smooths and coordinates muscle movement |
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what kind of neurotransmittor is dopamine?
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inhibitory
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in healthy individuals, dopamine relays signals from the substantia nigra to the next relay station, the:
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corpus stiatum
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what produces purposeful muscle activity
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balance of inhibitory dopamine (extrapyrimidal) & excitatory ACh (pyrimidal) mediated neurotransmission
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pathophysiology of PD
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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 |
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primary PD is AKA
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paralysis agitans
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is the cause of primary PD known?
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no (idiopathic)
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is primary PD curable?
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no - treatment is palliative
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what are the causes of secondary PD?
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drugs (iatrogenic - reversible)
poisoning infectious others |
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drugs that induce secondary PD
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reserpine
haloperidol chlorpromezine |
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infectious causes of secondary PD
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encephalitis
syphilis |
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other causes of secondary PD
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arterioschlerosis
neurodegenerative processes |
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objective of PD treatment
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to improve quality of life
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what are the 2 types of drugs used to treat PD
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dopaminergic agonists
cholinergic antagonists (for mild symptoms - tremors) |
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brand name for diphenhydramine
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benadryl
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what effect does diphenhydramine have?
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antihistaminic
some anticholinergic activity drowsiness CNS depression alleviates some symptoms of PD |
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brand name for benztropine mesylate
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cogentin
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what 3 effects does benztropine have?
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anticholinergic
antihistaminic local anaesthetic |
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benzotropine has similar potency and side effects as what drug?
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atropine
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benztropine should not be used in patients with:
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glaucoma
BPH |
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benign prostratic hyperplasia
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the prostate is enlarged, which pinches the urethra causing painful urination
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what are the common structural features of aminoalcohols
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bulky groups in the vicinity of hydroxyl and cyclic amino functional groups
gamma-aminopropanol arrangement |
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tertiary amines used to treat:
quaternary amines used for: |
PD
antispasmodic |
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what is the brand name for biperiden
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akineton
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what ring structure does biperiden have?
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piperidine ring
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biperiden is used to treat
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all forms of PD
spastic disorders (spinal cord injury, cerebral palsey, multiple schlerosis) akinesia, rigidity, tremor |
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brand name for procyclidine HCl
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kemadrin
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characteristics of procyclidine
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pyrrolidine ring
tertiary amine - PD |
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brand name for trihexyphenidyl HCl
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artane
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chracteristics of trihexyphenidyl
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piperidine ring
used in PD 1/2 as potent as atropine good margin of safety |
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brand name for isopropamide iodide
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darbid
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isopropamide used to treat?
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peptic ulcers
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DOA of isopropamide
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12 hrs
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isopropamide is contraindicated for patients with:
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glaucoma
BPH |
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brand name for ethopropazine HCl
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parsidol
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ring in ethopropazine
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phenothiazine
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ethopropazine used to treat:
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PD (controls rigidity, tremors, sialorrhea, oculogyric crises)
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side effects of ethopropazine?
contraindication? |
xerostomia
mydriasis CI: glaucoma |
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papaverine is a derivative of what plant?
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papaver somniferum
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papaverine has what kind of structure
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benzylisoquinoline
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MOA of papaverine
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generalized smooth muscle relaxation
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papaverine used to treat
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peripheral vascular diseases (spasmolytic activity)
male impotency |
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papaverine not used often b/c?
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lack of potency
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what is raynaud's disease
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vascular disease
cyanosis of fingers, nails b/c of impaired blood flow |
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what are the 2 types of nicotinic antagonists
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ganglionic blocking agents
neuromuscular blocking agents |
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what are the 3 kinds of ganglionic blocking agents?
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depolarizing
nondepolarizing competitive nondepolarizing noncompetitive |
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what are the 2 kinds of neuromuscular blocking agents?
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nondepolarizing
depolarizing |
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what was the 1st class of drugs used for hypotensive effect?
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neuromuscular blockers
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a drug that blocks the sympathetic system is known as:
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sympathoplegia
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a drug that blocks the parasympathetic system is known as:
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parasympathoplegia
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what affects do sympathoplegia drugs have?
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orthostatic hypotension
sexual dysfunction |
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what affects do parasympathoplegia drugs have?
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constipation
dry mouth blurred vision precipitation of glaucoma |
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in what NS do ganglionic blockers work? neuromuscular blockers?
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autonomic
somatic |
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what stimulant is a depolarizing ganglionic blocking agent?
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nicotine
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at low doses, nicotine is a _______; at high doses, it is a ________
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stimulant (depol & repol)
ganglionic blocker (no repolarization) |
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what therapeutically useful drugs are there in the depolarizing gangionlic blockers group?
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none
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MOA of nondepolarizing comkpetitive ganglionic blocking agents
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bind to nicotinic receptor but lack intrinsic activity for impulse transmission (unable to depolarize the cell)
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name 5 examples of nondepolarizing competitive ganglionic blocking agents
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tetramethylammonium salts
hexamethonium trimethaphan mecamylamine |
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what is the difference between hexamethonium and decamethonium
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hexa: 6c, strong ganglionic blocker, weak curariform activity
deca: 10c, weak gang blocker, strong curariform activity |
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brand name for trimethaphan camsylate
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arfonad
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what ring structure does trimethaphan camselate have?
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camphor sulfonate
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DOA of trimethaphan
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short, 10-30 min
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use for trimethaphan
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used in emergency room to lower BP (given by iv, inactive orally)
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brand name for mecamylamine
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inversine
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what ring structure does mecamylamine have?
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norbornane ring
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what is mecamylamine rarely used?
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causes severe orthostatic hypotension
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curariform activity AKA
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neuromuscular blocking activity
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what is a NMJ?
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specialized synapse between a motor neuron and skeletal muscle
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when are neuromuscular blocking agents commonly used?
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during surgical procedures as adjuncts to general anesthesia
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what are NM blocking agents used during surgery?
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induce reversible paralysis
no central activity |
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what is the prototype for nondepolarizing NMJ blockers?
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d-tubocurarine
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example of a depolarizing NMJ blocker
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succinylcholine
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tubocurarine is derived from what plant?
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curare (chondodendron tomentosum)
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what is the half life of tubocurarine?
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90 min
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DOA of tubocurarine
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2 hrs (binds at receptor for only 1 msec)
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uses for tubocurarine
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adjunct in general anesthesia
arrow poison |
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the brand name for atracurium besylate
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tracrium
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DOA of atracurium?
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short - 20min b/c easily hydrolyzed by plasma esterases
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what 2 ring structures does atracurium have?
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benzyl
tetrahydroisoquinoline |
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which is more potent: atracurium or tobocurarine?
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atracurium, 2.5x
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uses for atracurium?
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skeletal muscle relaxant for short surgical procedures
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paralysis caused by atracurium can be reversed by? how?
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AChEI - incr amount of ACh present, competes with drug for receptor
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why can atracurium be dangerous if you are on it for a long time?
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metabolyte can accumulate in the brain & cause seizures
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what is laudanosine?
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breakdown product of atracurium
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what is the brand name for doxacurium cl?
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nuromax
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what ring complex does doxacurium have?
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benzylterahydroisoquinoline
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what is the difference between atracurium & doxacurium?
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doxa has an extra methoxy group - hinds access of esterases - longer doa
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uses for doxacurium
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skeletal muscle relaxant for surgical procedures lasting longer than 90 min
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what is the brand name for pancuronium bromide?
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pavulon
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what ring complex does pancuronium have?
|
amino steroid
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what 2 placess does pancuronium act?
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nicotinic receptor
ion channel |
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which is more potent: tubocurarine or pancuronium?
|
pancuronium, 5x
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uses for pancuronium
|
skeletal muscle relaxant during surgery
adjunct to anesthesia |
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what are the possible metabolytes of pancuronium?
|
3-OH
17-OH 3,17-dihydroxy |
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brand name for succinyl cl
|
anectine
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what class does succinly cl belong to?
|
depol NMJ blocker - only useful agent in its class
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doa of succinyl cl?
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very short acting
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succinyl cl is unstable in what kind of soln?
|
alkaline
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uses for succinyl cl
|
skeletal muscle relaxant in surgery
intratracheal intubation endoscopic procedures |
