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56 Cards in this Set

  • Front
  • Back
. Cholinergic drugs
drugs that work on aceteal choline
Direct acting cholinomimetics general description
aceteal choline mimincers-copy affects of aceteal choline
Cholinolytic pharmacology-
block affects of aceteal choline
Direct-acting cholinomimetics examples
a. Examples; bethanechol, pilocarpine, and nicotine
. Pharmacodynamics/mechanism of action of direct acting cholinomimetics
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
. 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
nictoine:
Direct-acting cholinomimetics
b. Pharmacodynamics
nicotine used for treatment of cigarette
withdrawal symptoms
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
. Indirect acting cholinomimetics
a. examples:
neostigmine (does not pass blood
brain barrier; BBB) and donepezil (Aricept; passes BBB and produces central effects)
indirect acting cholinomimetics
pharmacodynamics
mechanism of action: acetylcholinesterase
inhibitors; ACh accumulates in synapse and
produces a cholinergic response
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
how Neostigma is used for myesthenia
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
. Cholinolytic pharmacology

a. Examples:
atropine and scopolamine
cholinolytic . Pharmacodynamics

mechanism of action:
muscarinic cholinergic receptor antagonists
cholinolytic therapeutic effects
scopolamine: used in the treatment of motion
sickness; inhibits cholinergic activation of
emesis center
Emesis=vomit center
Pharmacotoxicology of cholinolytics
cholinolytics suppresses
PNS functions
Ganglionic blockers
example;
mecamylamine
ganglionic blockers pharmacodynamics mechanism of action:
nicotinic cholinergic receptor
antagonist for ANS
ganglionic blcockers theraputic effect
: used in the treatment of severe hypertension
Skeletal muscle relaxants/anti-spastic pharmacology

a. Examples:
baclofen; pancuronium; succinylcholine;
and botulinum neurotoxins
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
. 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
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
Therapeutic effects

pancuronium and succinlycholine
induce
skeletal muscle relaxation needed during
surgery, tracheal intubations, and
electroconvulsant shock therapy
therapuetic effects
botulinum neurotoxins
induces skeletal muscle
paralysis at injection sites, used for the
cosmetic removal of facial wrinkles
. drugs that alter the
biosynthesis of catachol-
amines

(1). examples:
methyl-
tyrosine; L-DOPA
). 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
therapeutic effects: methyl-tyrosine:
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
therapeutic effects of L_DOPA
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
. generalized sympathomimetics examples
epinephrine and dopamine
mechanism of action: epinephrine and dopamine
). 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
). 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 (beta2 AR agonist activity induces bronchiodilation, alpha1 AR agonist induces peripheral vasoconst-riction which is effective against circulatory shock
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
selective alpha adrenergic receptor sympathomimetics

(1). examples:
phenylephrine, tetrahydralazine and
clonidine
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)
). therapeutic effects:

phenylephrine
can be used as a nasal
decongestant by inducing vasoconstriction of blood vessels in nasal mucosa
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
therapeutic effects clonidine
is used as an antihypertensive drug
. selective beta adrenergic receptor sympathomimetics

(1). examples:
isoproterenol, dobutamine, albuterol, and ritodrine
. selective beta adrenergic receptor sympathomimetics mechanism of action
isoproterenol is a
generalized beta1,2
adrenergic receptor
agonist; dobutamine
is a selective beta1 AR
agonist; albuterol and ritodrine are selective beta2 AR agonists
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
Indirect acting and mixed acting sympathomimetics

(1). examples:
amphetamines and ephedrine
). 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
therauptic effect Amphetamines:
CNS stimulants that is used to treat narcolepsies, minimal brain disorder in elderly and attention deficit disorders
therauptic effect Ephedrine
used as a nasal decongestant and bronchioldilator of airway, but membranes are constricted so membranes are thin
Selective alpha adrenergic receptor sympatholytics

(1). examples:
phentolamine and prazosin
). 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
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
theraputic effects prazosin
used as an anti-
hypertensive drug; reduces
peripheral vasoconstriction
to renal and mesenteric
vascular beds
Selective beta-adrenergic receptor sympatholytics

(1). examples
propranolol and metaprolol
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”
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)
pharmacotoxicology of adrenergic drugs

a. sympathomimetics
: CNS agitation, tremors, insomnia, hypertension, pressure headaches, etc.
pharmacotoxicology of sympatholytics
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
what cancels out ephedrine
antagonistic interactions, e.g. ephedrine +
propranolol. They’d cancel e/o out!
what is bad to mix with prazosin
additive interactions, e.g. prazosin + propranolol- both lwoer BP so you get extremly hyptoensive