Term
| Possible effects of drugs on synthesis of transmitter, and how it affects receptor activation |
|
Definition
Increased synthesis of T - Increase
Decreased synthesis of T - Decrease
Synthesis of super t - increase |
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Term
| Possible effects of drugs on storage of transmitter + effects on receptor activation. |
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Definition
| Reduced storage of T - Decrease |
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Term
| Possible effects of drugs on release of transmitter + effects on receptor activation |
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Definition
promotion of T release - Increase
Inhibition of T release - Decrease |
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Term
| Possible effects of drugs on receptor binding + effects on receptor activation |
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Definition
Direct receptor activation - Increase
Enhanced response to T - Increase
Blockade of T binding - Decrease |
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Term
| Possible effects of drugs on termination of transmission |
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Definition
Blockade of T reuptake - Increase
Inhibition of T breakdown - Increase |
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Term
| Functions of parasympathetic nervous system |
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Definition
Slowing of heart rate
Increased gastric secretion
emptying of bladder
emptying of bowel
focusing the eye for near vision
constricting the pupil
contracting bronchial smooth muscle
cranio-scral outflow of spinal cord. |
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Term
| Functions of the sympathetic nervous system |
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Definition
Regulating the cardiovascular system
Regulating body temp
Implementing fight or flight
thoraco-lumbar outflow |
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Term
| Characteristics of fight or flight |
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Definition
Increasing heart rate and blood pressure
Shunting blood away from skin and viscera and into skeletal muscles
Dilating the bronchi to improve oxygenation
dilating the pupils
mobilizing stored energy |
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Term
| Transmitter released by all preganglionic neurons/somatic motor system neurons |
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Definition
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Term
| Neurotransmitter released by Sympathetic postglangionic neurons |
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Definition
NE to various organs
ACh to sweat glands
Epi from adrenal medulla |
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Term
| Nicotinic(N) receptor location and response to activation |
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Definition
| All autonomic NS ganglia and the adrenal medula. Receptor activation results in stimulation of parasympathetic and sympathetic postganglionic nerves and the release of epinephrine from the adrenal medula. |
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Term
| Nicotinic(M) receptor location and response to activation |
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Definition
| located in the neuromuscular junction. Activation results in skeletal muscle contraction. |
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Term
| Muscarinic receptor locations and function |
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Definition
Eye - contraction of ciliary muscle focuses for near vision. Contraction of iris sphincter causes miosis (decreased pupil diameter).
Heart - decreased rate
Lung - constriction of bronchi/promotion of secretions
Bladder - Contraction of detrussor increases bladder pressure. Relaxation of trigone sphincter allows urine to leave the bladder. Coordinated contraction leads to bladder emptying.
GI Tract - salivation, increased gastric secretions, increased intestinal tone and motility, Defecation
Sweat glands (innervated by sympathetic) - generalized sweating
Sex organs - erection
Blood vessels (not actually innervated by sympathetic neurons) - vasodilation. |
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Term
| Alpha(1) receptor location and response to activation |
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Definition
Eye - contraction of radial muscle of the iris causes mydriasis (increased pupil size).
Arterioles (skin, viscera, mucous membranes) - constriction
Veins - constriction
Sex organs, male - ejaculation
Prostatic capsule - contraction
Bladder - contraction of trigone and sphincter |
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Term
| Alpha (2) receptor location and response to activation |
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Definition
presynaptic nerve terminals - inhibition of release
**Alpha 2 receptors in the central nervous system are postsynaptic. |
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Term
| Beta (1) receptor location and response to activation |
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Definition
Heart - increased rate/force, increased AV conduction velocity.
Kidney - release of renin (net effect = increased bp) |
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Term
| Beta (2) receptor location and response to activation |
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Definition
Arterioles (heart, lung, skeletal muscle) - Dilation
Bronchi - Dilation
Uterus - relaxation
Liver - Glycogenolysis
Skeletal muscle - enhanced contraction, glycogenolysis |
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Term
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Definition
| Kidney - Dilation of kidney vasculature |
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Term
| Adrenergic receptor subtypes activated by epinephrine |
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Definition
| Alpha1,Alpha2, Beta1, Beta2 |
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Term
| Adrenergic receptor subtypes activated by norepinephrine |
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Definition
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Term
| Adrenergic receptors activated by Dopamine |
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Definition
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Term
|
Definition
| enzyme that breaks down acetylcholine |
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Term
|
Definition
| enzyme that inactivates NE |
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Term
|
Definition
| primarily through hepatic metabolism |
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Term
| Salagen (pilocarpine), what would be some SE at high doses? |
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Definition
Cholinomimetic (Cholinergic agonist)
muscarinic agonist
At therapeutic doses intended to increased production of saliva, main adverse effect is sweating. At high doses it can produce all muscarinic effects.
Side effects would be: contraction of cilliary & iris, decrease HR, constriction of the bronchi, voiding, and increase gastric motility, sweating, erection, and vasodilation. |
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Term
| Atropine - method of action and results of therapeutic dose |
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Definition
ParasympathoLYTIC (anticholinergic/antimuscarinic)
muscarinic antagonist. functions through competetive blockade of muscarinic receptors.
Influences mainly - heart, exocrine glands, smooth muscles, and eye
Increase heart rate, decreased secretion, relaxation of bronchi, decreased bladder detrusor tune, decreased tone and motility of GI.
Eye - mydriasis (dilation of pupil), cyclopegia (relaxation of ciliary muscle) = lens focused for far vision. |
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Term
| Atropine adverse effects and antidote |
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Definition
xerostomia (dry mouth), blurred vision, photophobia, increased intraocular pressure, urinary retention, constipation, tachycardia, abhidrosis (lack of sweat), thickening and drying of bronchial secretions. CNS effects - delerium, hallucinations.
Antidote - phygostigmine - reversable cholinesterase inhibitor. |
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Term
| Neuromuscular blocking agents |
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Definition
prevent ACh from activating nicotinic(m) receptors on skeletal muscles.
Nondepolarizing - bind competetively (turbocurarine, pencuronium, rocunorium, vecuronium.
Depolarizing - mimic ACh at NMJ. It gets metabolized much more slowly then ACh, Affected muscles lose the ability to contract after induced NM stimulation for 5-10 mins (initial contraction then relaxation).
succynylcholine (ultra-short acting) used for intubation, ECT
*Commonly used in surgeries but No analegesic, sedative, or amnestic properties. |
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Term
| Catecholamines; what is there function |
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Definition
Adrenergic agonist
Norepi, epi, isoproterenol, dopamine, dobutamine
Broken down by COMT & MAO (monoamine oxidase).
Available in IV only
short duration
do not cross BBB |
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Term
| Noncatecholamines; what is its function |
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Definition
Is a adrenergic agonist
ephedrine, phenylephrine, terbutaline
metabolized slowly by MAO
could be used orally, longer 1/2 life, can cross BBB |
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Term
| Which receptors do Isoproterenol and Dobutamine activate? |
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Definition
Isoproteternol - b1 and b2
Dobutamine - B1 |
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Term
| Which receptors do ephedrine, phenylephrine, and terbutaline activate |
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Definition
Ephedrine - a1,2 b1,2
phylnephrine - a1
terbutaline - b2 |
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Term
| Alpha 1 receptor agonists therapeutic uses and adverse effects |
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Definition
elevate bp, mydriasis (pupil dilation), hemostasis, nasal decongestion, adjunct to local anathesia (slows rate of absorption).
adverse effects - hypertension, necrosis (extravasation), bradycardia (vasoconstriction increases BP triggers baroceptor reflex triggered in response to high BP to decrease HR. |
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Term
| Clinical use for Alpha 1 antagonist |
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Definition
| treatment of hypertension (dilation), and benign prostatic hyperplasia (relaxation). tumour in adrenal medula, Raynaud's disease (spasm of the arterioles in the extremities) |
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Term
| Phentolamine vs prazosin/terazosin |
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Definition
phentolamine is a non selective alpha adrenergic blocking agent. Produces a1 and a2 blockade.
prasozin, terazosin are selective for a1 |
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Term
|
Definition
alpha1 blocker.
Adverse effects related to alpha 1 blockers:
racing heart, dizziness, stuffy head/congestion...
explained by:
orthostatic hypotension - profound first dose hypotension
reflex tachycardia
nasal congestion
ED
sodium retention |
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Term
| Beta 1 receptor activation, therapeutic uses and adverse effects |
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Definition
Uses -
cardiac arrest, heart failure, shock, atrioventricular shock
Adverse effects
- tachycardia, dysrrhythmias, angina pectoris (from increased O2 demand) |
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Term
| Beta 2 receptor activation: therapeutic uses and adverse effects |
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Definition
Uses - Asthma, Delay preterm labor
Adverse effects -
effects of glucose? Causes hyperglycaemia because breaks down glycogen to glucose (glycogenlysis).
tremors (enhanced skeletal muscle contaction).
decreased potassium |
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Term
| Beta 1 antagonism clinical uses |
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Definition
Treatment of angina (decreases rate and force)
Treatment of Dysrhythmia - decreased conduction |
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Term
| Beta 2 antagonism clinical uses |
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Definition
| Side effect = exacerbation of PVD (peripheral vascular disease), asthma, hypoglycemic unawareness |
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Term
|
Definition
nonselective - activate b1 and b2 receptors. E.x. propranolol
Cardioselective (to a certain dose)
blocks beta 1 (metaprolol)
Blockade of beta and alpha 1
- Carvedilol
ISA (intrinsic sympathomimetic activity)
acebutalol - partial agonist at beta receptors. |
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Term
| Dopamine therapeutic uses |
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Definition
| Dilates renal vasculature, enhances cardiac performance (activation of b1) |
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Term
Filtration in the glomerulus:
Reabsorption: |
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Definition
electrolytes, amino acids, drugs, metabolic wastes. Is a nonselective process.
Reasorption: occurs in the proximal convoluted tubule, loop of henle, and distal convoluted tubule. This is a selective process. Most diuretics will work to inhibit this. 99% of filtrate goes undergoes reabsorption.
Active tubular secretion: Occurs in proximal convoluted tubule. Selective pump for organic acids and bases (wastes, drugs, and toxins). |
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Term
| Aldosterone in Kidney, where is it released from |
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Definition
A mineral corticoid of the adrenal cortex. Stimulates NA+ reabsorption from the distal nephron.
causes K+ loss |
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Term
| ADH, what happens in deficiency & excess? |
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Definition
acts at collecting duct - makes it more permeable to H2O
In deficiency there is dilute urine (DI), and in excess is concentrated urine (SIADH). |
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Term
|
Definition
low ceiling (after you titrate past a particular concentration and it will have no further effect), thiazide diuretic.
Commonly found with ACE-1 inhibitor
used for hypertension, mild-moderate edema.
Blocks reabsorption of Na+,Cl-, K+, and H20 in early segment of the distal convoluted tubile
10% of filtered Na load. |
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Term
|
Definition
loop diuretic, high ceiling
Affects ascending loop of henle, 20% of filtered Na+ Cl- load = more profound diuresis
Oral* potential for decreased efficacy in edematous states and patients with renal dysfunction and uremia
Uses
Edematous states, pulmonary edema, hypertension |
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Term
|
Definition
| K+ sparing diuretic. Aldosterone antagonist (would decrease Na+ reabsorption and increase the K+). Works at collecting and late distal tubule. Can cause synthesis of Na+-K+ pumps. |
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Term
| Common mechanism for Diuretics |
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Definition
Blocking Na+ and Cl- reabsorption.
More solute in nephron, creates osmotic pressure and prevents passive reabsorption of water.
most act on luminal surface of tubular cells. |
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Term
|
Definition
| can keep increasing dose to achieve more diuresis |
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Term
|
Definition
maximal effects occur at low doses
titrating the dose above |
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|
Term
| If you have a patient who has a need for a more profound diuretic response, which type of diuretic would you use? |
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Definition
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Term
| Thiazides adverse effects |
|
Definition
Hypokalemia* - most common cause
•Mechanism?: aldosterone secretion compensating for
fluid loss, ↑ reabsorption of Na+ & H2O to the collecting
duct enhances potassium (and hydrogen) losses
• Hyperuricemia
• Hyponatremia
• Hypomagnesemia
• Hypercalcemia – not usually significant
•In contrast loops cause hypocalcemia |
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Term
| Allergy concerns with Thiazides |
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Definition
|
|
Term
| Loop Diuretic adverse effects (furosomide) |
|
Definition
Hypotension
• Hypokalemia** - can be severe
• Hyponatremia
• Hypochloremia
• Ototoxicity (rare)
• IV, rapid infusion
• Caution with other drugs that can cause ototoxicity
• Hyperglycemia
• Hyperuricemia
• Hyperlipidemia
• Hypocalcemia (different than thiazides)
• not usually significant because Ca+ is actively reabsorbed at the distal convoluted tubule |
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Term
| Aldosterone antagonists AKA - K+ sparing Diuretics. |
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Definition
Spironolactone (Aldactone)
• Aldosterone antagonist
•@ collecting & late distal tubule
• Can cause synthesis of Na
+
/K+
pumps
Uses - edematous states (delayed, minor diuresis)
•Delay in onset of effect - due to time required to
synthesize Na+/K+ transporters
•Diuresis – minimal because filtered Na+
load remaining
•Current practice
• Severe heart failure – mechanism? |
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Term
|
Definition
Side effects
• Hyponatremia
• Hyperkalemia**
• Because of its steroid-like structure
• Body mistakes it for other hormones
• Gynecomastia (enlargement of mens breasts), menstrual irregularities, hirsutism (growth of hair on face),
deepening of the voice. |
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Term
| Adverse effects of Diuretics as a group |
|
Definition
Hypovolemia
Acid-Base imbalance
Electrolyte imbalances |
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Term
| Interactions for diuretics in general |
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Definition
Pharmacokinetic (drug/drug, drug/disease, drug/food)
Pharmacodynamic (drug/drug, drug/disease, drug/food)
• interactions that affect/cause:
• diuresis
• electrolyte abnormalities
• blood pressure
• renal blood flow
Interactions could be additive or opposite |
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Term
|
Definition
Study of drugs that alex processes controlled by the nervous system.
Agents (drugs and toxins) act on the peripheral NS or CNS. |
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|
Term
Dual opposing, and Dual complimentary:
Single innervation: |
|
Definition
Dual opposing= When the sympathetic and parasympathetic work on the same area with opposite effects (ex. sympathetic increases HR, parasympathetic decreases HR).
Dual Complimentary= Para and Sym work on the same area with similar effects (ex. erection controlled by para and ejaculation controlled by sym).
Single innervation is when only one of the two works on a area (ex. only sympathetic has any effects on the BV). |
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Term
| What is the difference between drugs that effect/block electrical conduction, compared to drugs that effect neurotransmitter transmissions: |
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Definition
Drugs that effect electrical conduction will have the same effect in all nerves, and will be non-specific. Effecting the nerves axons.
Drugs that effect neurotransmitter transmission will have selectivity. |
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|
Term
| What are the 5 steps to synaptic transmission? |
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Definition
| Synthesis, storage, release, receptor binding, termination. |
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|
Term
| Physostigmine: What is its effects, what would this be used for, what is effects is this similar to, what are the two categories of this? |
|
Definition
This is a cholinesterase inhibitor (enzyme that breaks down ACh at the post synaptic terminal). This could be used for a Atropine overdose (muscarinic antagonist). The cholinesterase inhibitor has the same effects as a muscarinic agonist would have.
The two categories are reversible or irreversible inhibiting. |
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Term
|
Definition
| Treat hypertension, and mobilize fluids in oedematous states (heart failure, cirrhosis, and renal disease). |
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