Nervous System Flashcards
muscarinic antagonists
atropine
muscarinic agonists (parasympathomimetic)
bethanechol
ganglionic-stimulating agents
nicotine
cholinesterase inhibitors (ChE)
physostigmine, neostigmine
neuromuscular-blocking agents
tubocurarine
adrenergic agonists (sympathomimetic)
epinephrine (adrenaline)
adrenergic antagonists (block alpha and beta receptors)
prazosin (alpha adrenergic antagonist), propanolol (beta adrenergic antagonist)
nicotine receptors
release of epinephrine from adrenal medulla; located at neuromuscular junction of skeletal muscle; causes skeletal muscle contraction
muscarinic receptors
decreased secretions from lungs, stomach, intestines, sweat glands; decrease in HR; smooth muscle contraction in bronchi and GI tract; miosis (sphincter contraction) and accommodation (ciliary contraction); voiding due to contraction of detrusor muscle and relaxation of trigone and sphincter muscles
alpha 1 receptors
mydriasis d/t radial muscle contraction; veins and arterioles are activated to constrict; decreased peripheral resistance and increased blood pressure; male sex organs are activated to promote ejaculation; contraction of prostatic capsule, trigone, and sphincter muscles
dopamine receptors
dilates blood vessels in the kidneys
beta 1 receptors
predominant receptor found on the heart; decreased HR, increased contraction force, and increased conduction through AV node; increased lipolysis; release of renin by the kidneys
beta 2 receptors
dilates bronchi; relaxes uterine smooth muscle; vasodilation of arterioles in heart, lungs, and skeletal muscle; slightly decreased peripheral resistance; increased glycogenolysis in the liver and muscles; skeletal muscle contraction
medications affecting the nervous system: general points
adaptive changes within brain with prolonged exposure; increased therapeutic effect; decreased side effects; tolerance and physical dependence; do not stop abruptly
Parkinson’s disease
treatment uses two main classes: medications that activate dopamine receptors (directly or indirectly) and medications that block acetylcholine receptors
seizure disorders
different types of seizures respond to different medications; usually require life-long management; medications must be discontinued slowly over 6 weeks to several months
schizophrenia
clinical course includes semi-remission punctuated by acute exacerbations; positive symptoms (agitation, delusions) medications: conventional antipsychotic [thorazine], atypical antipsychotic [clozapine]; negative symptoms (social withdrawal, poor self-care) medications: atypical antipsychotic [clozapine]; cognitive symptoms (difficulties with memory and learning); initial doses are high and given throughout the day; Maintenon doses given at bedtime
depression
symptom relief can take 1 to 3 weeks and possibly 2 to 3 months; three main groups: tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), and monoamine oxidase inhibitors (MAOIs)
bipolar disorder
typically managed with mood stabilisers; antipsychotics and antidepressants may be used during acute episodes of mania or depression; lithium, valproic acid [Depakote], and carbamazepine [Tegretol]
cholinesterase inhibitors: expected action
prevents ACh degradation; increased transmission of nerve impulses by increased ACh
cholinesterase inhibitors: therapeutic uses
increased muscle strength by increasing ACh at neuromuscular junction in myasthenia gravis; reversal of nondepolarising neuromuscular blocking agents (tubocurarine)
cholinesterase inhibitors: adverse effects
excessive muscarinic stimulation; increased GI motility and secretions, bradycardia, and urinary urgency (side effect can be treated with atropine); cholinergic crisis: above plus respiratory depression from neuromuscular blockade
cholinesterase inhibitors: contraindications and precautions
pregnancy C; CI in obstruction of GI and GU systems; caution with seizures, asthma, bradycardia, hypotension, and peptic ulcer disease
cholinesterase inhibitors: interactions
tubocurarine: neostigmine reverse blockade; atropine: counteracts; succinylcholine: increased neuromuscular blockade
cholinesterase inhibitors: education
wear medic-alert bracelet
cholinesterase inhibitors: prototypes
neostigmine, physostigmine
neuromuscular blocking agents: expected action
block ACh at neuromuscular junction (doesn’t cross blood-brain barrier)
neuromuscular blocking agents: prototypes
nondepolarising: tubocurarine, pancuronium; depolarising: succinylcholine
neuromuscular blocking agents: therapeutic uses
control spontaneous respiration in ventilated patients; adjuncts to general anaesthesia; diagnose myasthenia gravis; succinylcholine for: electroconvulsive therapy (ECT), intubation, and endoscopy
neuromuscular blocking agents: adverse effects
hypotension from histamine release and ganglionic blockade; respiratory arrest; bradycardia and dysrhythmias; succinylcholine: low pseudocholinesterase activity causing apnea, malignant hyperthermia (dantrolene), pain, and hyperkalaemia
neuromuscular blocking agents: contraindications
pregnancy C; SCh: CI for hyperkalaemia (trauma, burns)
neuromuscular blocking agents: interactions
general anaesthetics; aminoglycosides and tetracyclines causing increased NM blockade; neostigmine and ChE inhibitors causing decreased nondepolarising and increased alpha depolarising
dopaminergics (anti-Parkinson’s): expected action
levodopa taken up and converted to dopamine; carbidopa augments levodopa by preventing conversion to dopamine in intestine and periphery (increased DA in CNS)
dopaminergics (anti-Parkinson’s): prototypes
levodopa, carbidopa, sinemet
dopaminergics (anti-Parkinson’s): therapeutic uses
symptomatic relief from dyskinesias
dopaminergics (anti-Parkinson’s): adverse effects
dyskinesias; discolouration of sweat and urine; nausea and drowsiness; orthostatic hypotension; psychosis (clozapine); activation of malignant melanoma
dopaminergics (anti-Parkinson’s): contraindications and precautions
cardiac and psychiatric disorders; CI melanoma; 2 weeks from MAOI; pregnancy C
dopaminergics (anti-Parkinson’s): interactions
proteins interfere with absorption and transport; conventional antipsychotics (haldol, compazine) decreased alpha; pyridoxine decrease alpha; MAOI cause hypertension; carbidopa, dopamine agonists, anticholinergics, COMT inhibitors and dopamine tea leaders increase therapeutic effects
COMT (catechol O-methyltransferase)
catechol O-methyltransferase; deactivates catecholamines (e.g. dopamine, norepinephrine, acetylcholine, epinephrine, serotonin, histamine, etc); found in post-synaptic cell membranes of adrenergic neurons where it degrades norepinephrine; also found in the gut
dopamine agonists (antiparkinson’s): expected action
act directly on dopamine receptors
dopamine agonists (antiparkinson’s): prototype
pramipexole, ropinirole, bromocriptine
dopamine agonists (antiparkinson’s): therapeutic uses
monotherapy early; combined with levodopa in later stages
dopamine agonists (antiparkinson’s): adverse effects
orthostatic hypotension; psychosis; sleep attacks; daytime sleepiness; dyskinesias; nausea
dopamine agonists (antiparkinson’s): contraindications and precautions
pregnancy C; caution with liver and kidney impairment
dopamine agonists (antiparkinson’s): interactions
levodopa can decrease motor-control fluctuations permitting lower dose; levodopa can also increases risk of orthostatic hypotension and dyskinesias
centrally acting anticholinergics (antiparkinson’s): expected action
block ACh at muscarinic receptors which helps maintain ACh and dopamine balance
centrally acting anticholinergics (antiparkinson’s): prototype
benztropine [Cogentin], trihexyphenidyl [Artane]
centrally acting anticholinergics (antiparkinson’s): adverse effects
nausea (take with food); atropine-like effects (e.g. dry mouth, blurred vision, mydriasis, constipation); antihistamine effects (e.g. sedation, drowsiness)
centrally acting anticholinergics (antiparkinson’s): contraindications and precautions
CI in narrow-angle glaucoma
antiviral (antiparkinson’s): expected action
stimulate dopamine release; prevent dopamine reuptake; may block cholinergic and glutamate receptors
antiviral (antiparkinson’s): prototype
amantadine
antiviral (antiparkinson’s): therapeutic uses
Parkinson’s disease