Pharm Basics Review Flashcards
Parasympathetic activation: GI, Bladder, Eye, Lung, Heart, Lacrimal glands, salivary gland, uterus, penis/clitoris
GI: increased digestion Bladder: wall contraction, relax sphincter Eye: mitosis, ciliary muscle contraction Lung: smooth muscle contraction Heart: decreased heart rate/contractility Lacrimal glands: stimulate tears Salivary gland: watery secretions Uterus: contraction Penis/clitoris: erection/engorgement
Cholinergic excess
Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle/CNS Lacrimation Salivation Sweating (DUMBBELSS)
organophosphate poisoning
inactivation of acetylcholinesterase -> excess cholinergic activation -> DUMBBELSS
Treatment of organophosphate poisoning
atropine - blocks muscarinic receptors
pralidoxime - regenerates acetylcholinesterase (give both)
Myasthenia gravis
Abs against acetylcholine receptor
most common presentation: ptosis & diplopia that worsens throughout the day
Tension test -> Edrophonium (autoAb test is more specific)
Myasthenia gravis in relation to thyroid pathology
50% associated with thymus hyperplasia
20% associated with thymic atrophy
15% associated with thymic tumor (thymoma)
What is myasthenia crisis?
rapidly progressing weakness especially in respiratory muscles
What is the treatment for myasthenia gravis?
indirect cholinergic agonist (acetylcholinesterase inhibitors)
immunotherapy
thymectomy
plasmapheresis
What are the symptoms of inhibiting parasympathetic activity?
Hot as a hare -> hyperpyrexia (not sweating)
Red as a beet -> flushing
Blind as a bat -> cycloplegia, mydriasis (lose accommodation)
Dry as a bone -> lack of salivation
Mad as a hatter -> delirium
Bloated as a toad -> constipation and urinary retention
Tacky as a polyester suit -> tachycardia
Which anticholinergics are used in the treatment of urge urinary incontinence?
oxybutynin tolterodine darifenancin trospium solifenacin
“Off The Darn Toilet Seat”
In what populations is atropine contraindicated?
BPH, hyperthermia, acute angle glaucoma, elderly, GI obstruction/ileus
What other medications have anticholinergic side effects?
- first generation H1 blockers: diphenhydramine (Benadryl), doxylamine (Unisom), chlorpheniramine
- Neuroleptics (thioridazine, chlorpromazine, clozapine, olanzipine)
- TCAs (amitriptyline)
- Amantadine
What does stimulation of the alpha1 receptors cause?
vascular smooth muscle contraction -> increased peripheral resistance, increased BP, mydriasis, increased bladder sphincter contraction
What does stimulation of the alpha 2 receptors cause?
stimulates beta cells of the pancreases, some smooth muscle cells, inhibits NE release
What does stimulation of the beta 1 receptors cause?
tachycardia, increased lipolysis, increased myocardial contractility, increased release of renin
What does stimulation of the beta 2 receptors cause?
vasodilation, slightly decreased peripheral resistance, brochodilation, increase lipolysis, increased insulin resistance, decreased uterine tone
Where does vesamicol act at the NMJ?
Vesamicol inhibits packaging of ACh into vesicles
Where does hemicholinium act at the NMJ?
inhibits the choline/Na+ transporter
Where does Black widow spider toxin act at the NMJ? What does it cause?
stimulates the release of ACh from the presynaptic terminal; causes spastic paralysis
Where does botulinum toxin act at the NMJ? What does it cause?
inhibits release of ACh from the presynaptic terminal; causes flaccid paralysis
outline the path of enzymes and cofactors required to convert phenylalanine to epinephrine.
phenylephrine + phenylalanine hydroxylase + BH4 -> Tyrosine + tyrosine hydroxylase + BH4 -> DOPA + DOPA decarboxylase + Vit B6 -> Dopamine + dopamine beta-hydroxyalse + Vit C -> NEpi + PNMT -> Epinephrine
Which enzyme is inhibited by cortisol in the conversion of phenylalanine to epinephrine?
PNMT (NEpi -> Epi)
What enzymes are responsible for metabolizing NEpi?
COMT (catechol-o-methyltransferases) and MAO (monoamine oxidase)
Where does reserpine act on the noradrenergic NMJ?
inhibits the packaging of NEpi into vesicles
Where does metyrosine act on the noradrenergic NMJ?
inhibits the enzyme tyrosine hydroxylase
What three enzymes inhibit the reuptake of NEpi?
cocaine, TCA’s, SNRIs
What three enzymes facilitate the release of NEpi?
amphetamines, ephedrine, tyramine
What two enzymes inhibit the release of NEpi?
guanethidine, bretylium (CCB for arrhythmia)
What presynaptic auto receptor stimulates the release of NEpi?
AT receptor (Angiotensin)