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56 Cards in this Set
- Front
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. Cholinergic drugs
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drugs that work on aceteal choline
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Direct acting cholinomimetics general description
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aceteal choline mimincers-copy affects of aceteal choline
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Cholinolytic pharmacology-
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block affects of aceteal choline
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Direct-acting cholinomimetics examples
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a. Examples; bethanechol, pilocarpine, and nicotine
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. Pharmacodynamics/mechanism of action of direct acting cholinomimetics
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mechanism of action: bethanechol and pilocarpine are muscarinic cholinergic receptor agonists; BIND TO MUSCARINIC RECEPTORS AND HAVE HIGH INTRINSIC ACTIVY
nicotine is a nicotinic cholinergic receptor agonist in the CNS, Mimic affect of ACH |
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. Direct-acting cholinomimetics
:. Pharmacodynamics therapeutic uses: |
bethanechol used in the
treatment of G-I and urinary bladder paralysis usually after a major trauma or surgery; pilocarpine used in treatment of glaucoma in form of eye drops |
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nictoine:
Direct-acting cholinomimetics b. Pharmacodynamics |
nicotine used for treatment of cigarette
withdrawal symptoms |
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1. Direct-acting cholinomimetics
c. Pharmacotoxicology: |
bethanechol can
induce systemic effects associated with diarrhea, incontinence, bradycardia, etc. exaggerated theraputic effect bc produces PS responses that you will see everywhere |
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. Indirect acting cholinomimetics
a. examples: |
neostigmine (does not pass blood
brain barrier; BBB) and donepezil (Aricept; passes BBB and produces central effects) |
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indirect acting cholinomimetics
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pharmacodynamics
mechanism of action: acetylcholinesterase inhibitors; ACh accumulates in synapse and produces a cholinergic response |
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Indirect acting cholinomimetics
b. Pharmacodynamics Therapeutic effects |
neostigmine used to treat G-I and urinary
bladder paralysis, glaucoma, myesthenia gravis, treatment of anticholingergic effects produced some drugs like phenothiazines(used to treat psychologic disorder like scitzo-); donepezil used to treat symptoms of Alzheimer's disease associated with loss of cholinergic control of short term memory |
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how Neostigma is used for myesthenia
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associated with the destruction of nicotinic
cholinergic receptors at NueralMusclarJunction. Have antibodies that destroy these respeotrs, so decreased muscle reaction. Neostigma is used to blose Achase-so increase ACH in nueral musclar junction, so even tho less receptors more ach |
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. Cholinolytic pharmacology
a. Examples: |
atropine and scopolamine
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cholinolytic . Pharmacodynamics
mechanism of action: |
muscarinic cholinergic receptor antagonists
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cholinolytic therapeutic effects
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scopolamine: used in the treatment of motion
sickness; inhibits cholinergic activation of emesis center Emesis=vomit center |
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Pharmacotoxicology of cholinolytics
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cholinolytics suppresses
PNS functions |
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Ganglionic blockers
example; |
mecamylamine
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ganglionic blockers pharmacodynamics mechanism of action:
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nicotinic cholinergic receptor
antagonist for ANS |
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ganglionic blcockers theraputic effect
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: used in the treatment of severe hypertension
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Skeletal muscle relaxants/anti-spastic pharmacology
a. Examples: |
baclofen; pancuronium; succinylcholine;
and botulinum neurotoxins |
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Skeletal muscle relaxants/anti-spastic pharmacology
Pharmacodynamics: mechanism of action: pancuronium and baclofen |
baclofen is a GABA receptor agonist that suppresses
motor neuron activity and nerve conduction pancuronium is a nicotinic receptor antagonist on skeletal muscle: nondepolarizing relaxation (blocks excitation-contraction coupling |
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. Pharmacodynamics:
mechanism of action: succinylcholine and botulinum neurotoxins |
succinylcholine activates the ACh receptor and causes
depolarization (depolarizing action) but it remains bound to the receptor and prevents twitch summation and a sustained contraction botulinum neurotoxins inhibit proteins that mediate ACh exocytosis and thus inhibit release of Ach |
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therapeutic effects:
baclofen: |
inhibits activity of motor neurons
associated with exaggerated motor reflex activity, spastic movement disorders, caused by multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, strokes, or head injuries |
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Therapeutic effects
pancuronium and succinlycholine |
induce
skeletal muscle relaxation needed during surgery, tracheal intubations, and electroconvulsant shock therapy |
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therapuetic effects
botulinum neurotoxins |
induces skeletal muscle
paralysis at injection sites, used for the cosmetic removal of facial wrinkles |
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. drugs that alter the
biosynthesis of catachol- amines (1). examples: |
methyl-
tyrosine; L-DOPA |
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). mechanism of action of . drugs that alter the
biosynthesis of catachol- amines |
methyl-tyrosine
inhibits tyrosine hydroxylase; L-DOPA serves as a substrate for dopamine synthesis |
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therapeutic effects: methyl-tyrosine:
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treatment of
pheochromocytoma, a tumor of the adrenal medulla, that is associated with excessive production of catacholamines and the development of severe hypertension. So it blocks dop to go to dopamine so cant make any catacholamines. Inhibits enzyme |
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therapeutic effects of L_DOPA
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L-DOPA passes the BBB and elevates
dopamine synthesis in the basal ganglia of CNS which reduces tremors and other motor disorders associated with Parkinsonism |
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. generalized sympathomimetics examples
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epinephrine and dopamine
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mechanism of action: epinephrine and dopamine
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). s a alpha 1 and 2 and beta 1 and 2 adrenergic receptor agonist which induces fight/flight responses;
dopamine is an agonist for D-1, beta-1 and then alpha-1 adrenergic receptors |
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). therapeutic uses:
epinephrine: |
used as eye-
drops induce mydriasis; used as a respiratory mists induces bronchiodilation used for the treatment of asthma; parenteral administration used in the treatment of cardiac arrest(beta1 AR agonist) and anaphylactic shock (beta2AR agonist activity induces bronchiodilation, alpha1 AR agonist induces peripheral vasoconst-riction which is effective against circulatory shock |
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therapeutic uses:
dopamine |
used to treat
cardiogenic shock by acting as a renal D1 receptor agonist that mediates mesenteric blood vessel vasodilation to increase renal blood flow (RBF) and prevents renal failure and the beta1 responses increase cardiac output |
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selective alpha adrenergic receptor sympathomimetics
(1). examples: |
phenylephrine, tetrahydralazine and
clonidine |
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selective alpha adrenergic receptor sympathomimetics
mechanism of action |
phenylephrine and
tetrahydralazine are alpha-1 AR agonists; and clonidine passes BBB and acts as an alpha2 AR agonist which reduces release of catacholamines and SNS tone (activity) |
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). therapeutic effects:
phenylephrine |
can be used as a nasal
decongestant by inducing vasoconstriction of blood vessels in nasal mucosa |
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therapeutic effects:
tetrahydralazine |
is used to treat irritation of
eyes induced by allergens, smoke, fatigue, etc. it "gets the red out” by inducing vasoconstriction of blood vessels on the surface of the cornea of the eye |
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therapeutic effects clonidine
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is used as an antihypertensive drug
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. selective beta adrenergic receptor sympathomimetics
(1). examples: |
isoproterenol, dobutamine, albuterol, and ritodrine
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. selective beta adrenergic receptor sympathomimetics mechanism of action
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isoproterenol is a
generalized beta1,2 adrenergic receptor agonist; dobutamine is a selective beta1 AR agonist; albuterol and ritodrine are selective beta2 AR agonists |
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therapeutic affects:
isoproterenol and dobutamine |
are cardiac
stimulants, used in the treatment of cardiac arrest and heart failure; albuterol is commonly used as a brochiodilator and ritodrine is used to reduce myometrial uterine contractions and prevent pre-term birth |
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Indirect acting and mixed acting sympathomimetics
(1). examples: |
amphetamines and ephedrine
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). mechanism of action:
amphetamine and ephedrine |
amphetamine is
transported into the sympathetic axon terminal where it displaces catachol- amines from internal stores, this effect results in the release of NE into synapse, indirect sympathomimetic; ephedrine also displaces NE from internal stores (slow displacement) and it is an alpha1 and beta2 AR agonist, mixed actions |
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therauptic effect Amphetamines:
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CNS stimulants that is used to treat narcolepsies, minimal brain disorder in elderly and attention deficit disorders
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therauptic effect Ephedrine
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used as a nasal decongestant and bronchioldilator of airway, but membranes are constricted so membranes are thin
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Selective alpha adrenergic receptor sympatholytics
(1). examples: |
phentolamine and prazosin
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). mechanism of action:
phentolamine and prazosin |
phentolamine
is a generalized alpha adrener- gic receptor (alpha AR1,2 receptors) ant- agonist and prazosin is a selective alpha1 AR receptor antagonist |
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therapeutic effects:
phentolamine |
is used in the
treatment of frost-bite and Raynaud's syndrome; it reduces cutaneous vasoconstriction and increases blood flow to the skin. Vasocstriction occurs with frost bite and reynauds syndrome. Alpha 1 causes constrictive and active. Leads to increased blood flow by blocking the vasocostriction by inhibiting alpha 1 |
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theraputic effects prazosin
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used as an anti-
hypertensive drug; reduces peripheral vasoconstriction to renal and mesenteric vascular beds |
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Selective beta-adrenergic receptor sympatholytics
(1). examples |
propranolol and metaprolol
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propranolol and metaprolol
(2). mechanism of action |
propranolol is a generalized
beta1,2 AR antagonist and metoprolol is a selective beta1 AR antagonist and since cardiac tissue has a high density of beta1 ARs, metaprolol has been described as “cardioselective” |
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therapeutic effects:
propranolol and metoprolol |
metoprolol used hypertension
propranolol is used for the prophylactic treatment of migraine headaches that are associated with vasodilation (BAR2 mediated?); treatment of stress responses (palpitations, etc.), hypertension (includes blockade of BAR1 mediated renin release); cardiac arrhythmias; and ischemic heart disease (pectoralis angina) |
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pharmacotoxicology of adrenergic drugs
a. sympathomimetics |
: CNS agitation, tremors, insomnia, hypertension, pressure headaches, etc.
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pharmacotoxicology of sympatholytics
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opposite effect hypotension, orthostatic bc can’t maintain blood pressure hypotension, fatigue, exercise intolerance, bronchioconstriction (especially with asthma, COPD's), bradycardia that can lead to cardiac failure, CNS depression
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what cancels out ephedrine
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antagonistic interactions, e.g. ephedrine +
propranolol. They’d cancel e/o out! |
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what is bad to mix with prazosin
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additive interactions, e.g. prazosin + propranolol- both lwoer BP so you get extremly hyptoensive
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