Autonomic and Cholinergic Rc Flashcards
• INVOLUNTARY • SYMPATHETIC (SANS) AND PARASYMPATHETIC (PANS) • HANDLES VISCERAL FUNCTIONS • 2 NEURONS IN SERIES • PRE- AND POST- GANGLIONIC • ALL PREGANGLIONIC release Ach
AUTONOMIC
NERVOUS SYSTEM
All pregang fibers release ____ in the ANS
Ach
• FIGHT OR FLIGHT • RUNS ON NOREPINEPHRINE • INCREASES CO, BP, RR, BLOOD FLOW, BG • DECREASES RBF, DIGESTIVE PROCESSES • FIRES AT ONCE • SHORT PRE-, LONG POST-
Sympathetic nervous system
• NORMAL MAINTENANCE AND ANABOLIC METABOLISM • INCREMENTAL ACTIVATION • VAGAL STIMULATION • LONG PRE-, SHORT POST-
Parasympathetic nervous system
- VOLUNTARY
- CONTROLS MOVEMENT, RESPIRATION, POSTURE
- ALWAYS EXCITATORY
- NO GANGLIA
SOMATIC NERVOUS SYSTEM
• SYNTHESIZE AND RELEASE ACH • ALL PREGANGLIONIC EFFERENT AND SOMATIC MOTOR FIBERS TO SKELETAL MUSCLE • MOST PARASYMPATHETIC POSTGANGLIONIC FIBERS
CHOLINERGIC
FIBERS
- RELEASE NOREPINEPHRINE
* MOST SYMPATHETIC POSTGANGLIONIC FIBERS
ADRENERGIC
FIBERS
A ____ is a molecule that induces a response by binding to receptor at site of relase
-Short duration, quick acting
Neurotransmitter
A ____ is a molecule released in bloodstream that travels to target to induce effect;
Long lasting, long time before it can take action
neurohormone
______RECEPTORS
NICOTINIC (GANGLIONIC)
MUSCARINIC
CHOLINERGIC
______ RECEPTORS
ALPHA
BETA
DOPAMINE
ADRENERGIC
Is a nicotinic receptor used to excite or inhibit?
Excite
______ muscarinic receptors: CNS EXCITATION,
GASTRIC SECRETION
M1 – NEURAL;
______ muscarinic receptors:CARDIAC AND NEURAL
INHIBITION
M2 – ATRIAL;
______ muscarinic receptors:
GASTRIC ACID, SALIVARY
SECRETION, GI CONTRACTION,
OCULAR ACCOMMODATION, VASODILATION
M3 – GLANDULAR/SMOOTH MUSCLE;
Para or symp NS?
- Mydriasis
- Reduced saliva flow
- Increased SV and HR
- Vasoconstriction
- Reduced peristalsis and secretion
- Glycogen to glucose
- Inhibition of bladder contraction
- Epinephrine release
Sympathetic NS
Para or symp NS?
- Miosis
- Stimulated salivary flow
- Decreased HR
- Bronchoconstriction
- Stimulates peristalsis and secretion
- Stimulates bile release
- Bladder constriction
Parasmyp
\_\_\_\_\_\_ drugs • PARASYMPATHOMIMETIC • DIRECT ACTING • BINDS DIRECTLY TO NACH(OS) AND MACH(OS) • INDIRECT ACTING • INHIBITS ACETYLCHOLINESTERASE • AMPLIFIERS OF ENDOGENOUS ACH
Cholinergic drugs
DIRECT ACTING
- GLAUCOMA TX
- CAUSES MIOSIS, LOWERS IOP
- DENTAL USE – RADIATION-INDUCED XEROSTOMIA
CHOLINERGICS• PILOCARPINE (SALAGEN®)
DIRECT ACTING
CHOLINERGICS
- POST-OPERATIVE URINARY RETENTION
- MOST RESISTANT TO CHOLINESTERASE
• BETHANECHOL (URECHOLINE®)
DIRECT ACTING
CHOLINERGICS
- SELECTIVE FOR M3
- MORE SELECTIVE FOR EXOCRINE GLANDS
- RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYN
• CEVIMILINE (EVOXAC®)
- USED FOR TREATMENT OF
- MYASTHENIA GRAVIS
- GLAUCOMA
- GI MOTILITY
- REVERSAL OF NEUROMUSCULAR BLOCKADE
- ANTICHOLINERGIC TOXICITY
- ALZHEIMERS
INDIRECT ACTING
CHOLINERGICS
•Used for Diagnosis of myasthenia gravis Doesn’t enter CNS (quaternary
amine)
Not routinely used for treatment, short t ½ (5 min)
Edrophonium (Tensilon®
What 3 drugs? •Mild-to-moderate Alzheimer’s disease More selective AChE for management of cognitive dysfunction.
Galantamine,
rivastigmine,
donepezil
Irreversible AChE Long lasting Insecticides Parathion, malathion Nerve agents Sarin, soman tabun, VX Novichok Agents
ORGANOPHOSPHATES
Once a bond between an organophosphate and Serine site on acetylcholinesterase is ______, it is permanently out of commission/destroyed
Aged
What are the muscarinic symptoms of cholinergic toxicity?
Sludge Dumbbels
Salivation Lacrimation Urination Diarrhea GI discomfort Emesis
Diarrhea Urination Miosis/muscles weak Bronchorrhea Bradycardia Emesis Lacrimation Salivation/sweating
What are the nicotinic symptoms of cholinergic toxicity?
MTWTF
Muscle cramps Tachycardia Weakness Twitching Fasciculations
(Drug treating cholinergic toxicity)
• REGENERATES ACHE; must be given before aging
PRALIDOXIME (2-PAM)
(Drug treating cholinergic toxicity)
– REQUIRES HUGE AMOUNTS
• MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT
NICOTINIC SX (PARALYSIS)
ATROPINE
•BINDS MUSCARINIC RECEPTORS, BLOCKS ACH •TERTIARY AMINES HAVE CENTRAL EFFECTS • ATROPINE, SCOPOLAMINE (SCOPACE®), BENZTROPINE (COGENTIN®), DICYCLOMINE (BENTYL®) •QUATERNARY AMINES – PERIPHERAL EFFECTS • GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM (SPIRIVA®) 37
ANTICHOLINERGICS
(anticholinergics) \_\_\_\_\_ AMINES HAVE CENTRAL EFFECTS • ATROPINE, SCOPOLAMINE (SCOPACE®), BENZTROPINE (COGENTIN®), DICYCLOMINE (BENTYL®)
TERTIARY Amines
(anticholinergics) • \_\_\_\_ amines– PERIPHERAL EFFECTS • GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM (SPIRIVA®)
QUATERNARY AMINES
- PROTOTYPICAL ANTICHOLINERGIC
- MUSCARINIC SELECTIVITY
- NO EFFECT S/P HEART TRANSPLANT
- INDICATIONS
- BRADYCARDIA
- OP TOXICITY – HUGE AMOUNTS NEEDED
- DON’T USE < 0.5MG IN ADULTS
- PARADOXICAL BRADYCARDIA
ATROPINE
Where does atropine work as far as muscarinic receptor?
Blocks M2
•FOUND IN HYOSCYAMUS NIGER (HENBANE) •TERTIARY AMINE •PRIMARY USE • MOTION SICKNESS • VOODOO ZOMBIFICATION
SCOPOLAMINE
• QUATERNARY AMINE, FEWER CENTRAL EFFECTS • USED TO DRY SECRETIONS • SURGERY • KETAMINE TREATMENT • ADJUNCT FOR REVERSAL OF NEUROMUSCULAR BLOCKERS - Doesn't mess with HR
GLYCOPYRROLATE
______ uses
• OPHTHALMOLOGY
• MYDRIASIS, CYCLOPLEGIA, Decreases INTRAOCULAR PRESSURE (IOP)
• GI/GU
• ANTISPASMODIC, ANTIDIARRHEAL, URINARY INCONTINENCE
• CARDIOVASCULAR
• VAGOLYTIC (INCREASES HEART RATE)
• SECRETIONS
• DECREASES ALL; SURGERY AND DENTAL USES
• ANTIDOTE
• REVERSAL OF CHOLINERGIC TOXICITY (ORGANOPHOSPHATE POISONING)
• PULMONARY
• COPD / ASTHMA TREATMENT (BRONCHODILATION)
ANTICHOLINERGIC
USES
_____ effectes
CNS: Drowsiness, amnesia, agitation, hallucinations, coma
scopolamine > atropine
Eye: Mydriasis, cycloplegia, reduced lacrimal secretion
CV: Tachycardia (vagal inhibition)
Respiratory: Bronchodilation, reduced airway secretions
GI: Decreased motility, xerostomia
ANTICHOLINERGIC EFFECTS
How many mg of nicotine is fatal?
40 mg (1 drop of pure liquid)
(NICOTINIC DRUGS_
• PARTIAL AGONIST/ANTAGONIST • LONG T½ AND HIGH AFFINITY FOR NACH(OS) • INHIBITS: • NICOTINE BINDING • WITHDRAWAL SYMPTOMS • DOPAMINE RELEASE
•VARENICLINE (CHANTIX®)
The following drugs are used as \_\_\_\_\_\_\_ • DEPOLARIZING SUCCINYLCHOLINE • NONDEPOLARIZING ROCURONIUM
Neuromuscular blockers
• OPENS SODIUM CHANNELS • ONSET ~ 60 SECONDS • DURATION ~ 5 MINUTES • 1.5 MG/KG IV (ACTUAL BODY WEIGHT) • MORE IF HYPOTENSIVE • CAUTION: HYPERKALEMIA! • DENERVATION SUPERSENSITIVITY - 2 Ach molecules fused together and blocks Na channels
SUCCINYLCHOLINE
- NONDEPOLARIZING
- ONSET ~60 SECONDS
- DURATION ~ 45 MINUTES
- 0.6 – 1.2 MG/KG
- NO SIGNIFICANT ADR
- REVERSAL AGENT
ROCURONIUM
