nervou system pharm
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- what is the prototype muscarinic antagonist
- atropine
- what is the antidote to muscarinic antagonists or anticholinergic blockade
- physostigmine
- what is atropine used for
-
preop
myriasis ete surgery
bradycardia
intestinal hyertonicity and hypermobility
muscarinic agonist poisoning - what is the antodote for muscarinic agonists or cholinergics
- atropine
- what is the prototye muscarinic agonist
- bethanacol
- what is bethanacol used for
- to treat urinary retention
- what are the primary uses of muscarinic agonists
-
GU and GI- primary indication is urinary retention;
also GI disorders involvong bowel paralysis - what is the most effective antidote to muscarinic poisoning
- physostigmine (a cholinesterase inhibitor)
-
muscarinic agonists -how given
and why - PO give by mouth only IV or IM can cause circulatory colapse
- AE of muscarinic agonists
-
Cv-orthostatic hypotension
GI-excessive gastric activity-salivation, diarrhea, gastric acid secretion
Resp- increases secretions and cause bronchospam
eyes-blurs vision - prototype reversible cholinesterae inhibitor
- neostigmine
- primary use of neostigmine
- MG
- what is the symptoms of reversible cholinesterase inhibitor OD
-
cholinergic crisis
muscarinic plus NM blockade - what is the drug of choice for a cholinergic crisis
- atropine and mechanical ventialtion and O2
- How is physostigmine different from neostigmine
-
it is not polar so it readily crosses cell membranes
- irreversible cholinesterase inhibitors
-
Inectisides
only one indication is glaucoma - what are the most beneficial responses to alpha blockers the result of
- blockade of a1 receptors on blood vessels which cause vasocnstriction
- primary use of alpha blockers
- BPH causes smooth muscles of the prostrate to relax
- 3 characteristics of catecholamines
-
cant be used orally
breif duration of action
cant cross the blood brain barrier - can catecholamines cross the blood brain barrier
- no because they are polar molecules
- what are the noncatecholamines and can they be given orally
- ephedrine, phenylephrine and terbutaline
- A1 therapeutic uses
-
hemostasis
mydriasis - What happens when you activate muscarinic receptors
-
eye-miosis and near vision
heart-decreases rate
lungs-promotes bronchocnstriction and secretion
Blood vessels-dilates
bladder-contracts, voids
GI-increase tone, motility, secretions, defecation
sex organs-erection
sweat glands - Why give dopamine
-
shock
improves cv performance
dilates renal blood vessels - therpaeutic uses of epinephrine
-
1. vasoconstriction-hemostasis, inc BP, delay absorption of anesthetics
2. eye-mydriasis
3. heart-overcome AV block, restore function in cardiac arrest
4.lung-bronchodilation
5. tx of choice for anaphylaxis - AE of epinephine
-
hypertensive crisis
dysrythmias
angina
necrosis
hyperglycemia - uses of ne and how is it different from epi
-
hypotension and cardiac arrest
does not activate beta2 receptors so does not cause hyperglycemia in DM -
isoproterenol (isuprel)
where does it act?
therapeutic uses -
only at beta receptors
1. CV-overcome Av block, restart heart, incr CO in shock
2. asthma-causes bronchodilation but use has been abandoned bc we have more b2 selective drugs
3. bronchospasm-during anesthetia - AE of Isoproterenol
-
tachydysrythmia
hyperglycemia
angina - MAO inhibitors
- intensify the effects of dopamine, isoproterenol, epi
- Dobutamine
-
beta1 selective
only use is heart failure -
phenylephrine
what type?
uses? -
noncatecholamine
nasal decongestion
increase BP
dilate pupil -
terbutaline (Brethine)
uses
adverse effects -
1.asthma by producing broncholdialtion via b2
selective for beta 2 receptors
2. preterm labor-relaxes uterine smooth muscle
AE if given in large enough doses can activate b1>tachycardia and
tremor is most common -
ephedrine
activates?
-
a1a2b1b2
limited use because direct and indirect and non selective
is noncatecholamine so can cross the BB barrier - what does activation of Nm receptors do
- contracts sketelal muscle
- what does activation of Nn receptors do
- promotes ganglioni transmission at all ganlia in PSNS and SNS and promotes release of epi from adrenal medulla
-
Effects of B1 activation
-
heart-increases force of contraction, velocity of conduction through AV node, HR
kidney-renin-vasocnstrict-incr BP - muscarinic activation
-
miosis and near vision
urination
slows heart rate
constricts bronchi, GI smooth muscle
erection
vasodilation
sweating, secretions - alpha 1
-
dilates pupil
ejaculation
contracts prostrate and bladder
vasoconstriction - contraindications to muscarinic agonists and cholinesterase inhibitors
-
1. PUD
2. Asthma
3. GU GI obstruction
4. coronary insufficiency
5. hyperthyroidism - antidote for irreversible cholinesterase inhibiors (organophosphates)
-
pralidoxamine(cant cross BB barrier)
also atropine
mechanical ventilation
diazepam - DOC for atropine and other muscarinic antagonists OD
- physostigmine--readily crosses mebranes and is a reversible cholinesterase inhibitor
- therapeutic goals of cholinesterase inhibitors
-
myasthenia gravis
glaucoma
alzheimers
reverse NDNM - reversible cholinsterase inhibitors
-
neostigmine
physostgmine
donazepil
edrophonium
pyridostigmine - NMBA action
- prevent acetylcholine from activating nicotinicM receptors on skeletal muscles causing muscle relaxation
- ganglionic blocking agent
-
mecalymine
resembles effect of muscarinic antagonists(dry mouth, blurred vision, anhydrosis, constipation, urinary retention, tachycardia, photophobia) plus orhtostatic hypotension - anticholinergic or muscarinic antagonists side effects
-
dry mouth
constipation
urinary retention
photophobia
blurred vision
tachycardia
anydrosis - depolarizing NMB prototype
-
succinocholine
***has no antidote***** - non depolarizing NMB protype
-
tubocurare
also ium drugs - AE succinylcholine
-
malignant hyperthermia
hyperkalemia
prolonged apnea - succinocholine vs NDNMB
-
1. very short duration; abates more rapidly than NDNMB
2. flaccid paralysis but with transient contractions proceeding it - antidote to succinylchoine OD
- THERE IS NONE!!!
- FUNCTIONS OF THE PARASYMPATHETIC ns
-
1. EMPTY BLADDER
2. EMPTY BOWEL
3. DECREASE HEART RATE
4.CONSTRICT PUPIL
5. CONSTRICT BRONCHIALS
6. INCREASE GASTrIC SECRETIONS
7. NEAR VISION FOCUS