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Pharmacology > Autonomic and Cholinergic Rc > Flashcards

Autonomic and Cholinergic Rc Flashcards

1
Q 
• INVOLUNTARY
• SYMPATHETIC (SANS) 
AND 
PARASYMPATHETIC 
(PANS)
• HANDLES VISCERAL 
FUNCTIONS
• 2 NEURONS IN SERIES
• PRE- AND POST-
GANGLIONIC
• ALL PREGANGLIONIC release Ach
A

AUTONOMIC

NERVOUS SYSTEM

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2
Q

All pregang fibers release ____ in the ANS

A

Ach

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3
Q 
• FIGHT OR FLIGHT
• RUNS ON 
NOREPINEPHRINE
• INCREASES CO, BP, RR, 
BLOOD FLOW, BG
• DECREASES RBF, 
DIGESTIVE PROCESSES
• FIRES AT ONCE
• SHORT PRE-, LONG POST-
A

Sympathetic nervous system

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4
Q 
• NORMAL MAINTENANCE 
AND ANABOLIC 
METABOLISM
• INCREMENTAL 
ACTIVATION
• VAGAL STIMULATION
• LONG PRE-, SHORT POST-
A

Parasympathetic nervous system

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5
Q
  • VOLUNTARY
  • CONTROLS MOVEMENT, RESPIRATION, POSTURE
  • ALWAYS EXCITATORY
  • NO GANGLIA
A

SOMATIC NERVOUS SYSTEM

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6
Q 
• SYNTHESIZE AND RELEASE ACH
• ALL PREGANGLIONIC EFFERENT AND SOMATIC 
MOTOR FIBERS TO SKELETAL MUSCLE
• MOST PARASYMPATHETIC POSTGANGLIONIC 
FIBERS
A

CHOLINERGIC

FIBERS

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7
Q
  • RELEASE NOREPINEPHRINE

* MOST SYMPATHETIC POSTGANGLIONIC FIBERS

A

ADRENERGIC

FIBERS

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8
Q

A ____ is a molecule that induces a response by binding to receptor at site of relase
-Short duration, quick acting

A

Neurotransmitter

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9
Q

A ____ is a molecule released in bloodstream that travels to target to induce effect;
Long lasting, long time before it can take action

A

neurohormone

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10
Q

______RECEPTORS
NICOTINIC (GANGLIONIC)
MUSCARINIC

A

CHOLINERGIC

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11
Q

______ RECEPTORS
ALPHA
BETA
DOPAMINE

A

ADRENERGIC

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12
Q

Is a nicotinic receptor used to excite or inhibit?

A

Excite

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13
Q

______ muscarinic receptors: CNS EXCITATION,

GASTRIC SECRETION

A

M1 – NEURAL;

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14
Q

______ muscarinic receptors:CARDIAC AND NEURAL

INHIBITION

A

M2 – ATRIAL;

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15
Q

______ muscarinic receptors:
GASTRIC ACID, SALIVARY
SECRETION, GI CONTRACTION,
OCULAR ACCOMMODATION, VASODILATION

A

M3 – GLANDULAR/SMOOTH MUSCLE;

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16
Q

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
A

Sympathetic NS

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17
Q

Para or symp NS?

  • Miosis
  • Stimulated salivary flow
  • Decreased HR
  • Bronchoconstriction
  • Stimulates peristalsis and secretion
  • Stimulates bile release
  • Bladder constriction
A

Parasmyp

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18
Q 
\_\_\_\_\_\_ drugs
• PARASYMPATHOMIMETIC 
• DIRECT ACTING
• BINDS DIRECTLY TO NACH(OS) AND MACH(OS)
• INDIRECT ACTING
• INHIBITS ACETYLCHOLINESTERASE
• AMPLIFIERS OF ENDOGENOUS ACH
A

Cholinergic drugs

19
Q

DIRECT ACTING

  • GLAUCOMA TX
  • CAUSES MIOSIS, LOWERS IOP
  • DENTAL USE – RADIATION-INDUCED XEROSTOMIA
A

CHOLINERGICS• PILOCARPINE (SALAGEN®)

20
Q

DIRECT ACTING
CHOLINERGICS

  • POST-OPERATIVE URINARY RETENTION
  • MOST RESISTANT TO CHOLINESTERASE
A

• BETHANECHOL (URECHOLINE®)

21
Q

DIRECT ACTING
CHOLINERGICS

  • SELECTIVE FOR M3
  • MORE SELECTIVE FOR EXOCRINE GLANDS
  • RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYN
A

• CEVIMILINE (EVOXAC®)

22
Q
  • USED FOR TREATMENT OF
  • MYASTHENIA GRAVIS
  • GLAUCOMA
  • GI MOTILITY
  • REVERSAL OF NEUROMUSCULAR BLOCKADE
  • ANTICHOLINERGIC TOXICITY
  • ALZHEIMERS
A

INDIRECT ACTING

CHOLINERGICS

23
Q

•Used for Diagnosis of myasthenia gravis Doesn’t enter CNS (quaternary
amine)
Not routinely used for treatment, short t ½ (5 min)

A

Edrophonium (Tensilon®

24
Q 
What 3 drugs?
•Mild-to-moderate Alzheimer’s 
disease
More selective AChE for 
management of cognitive 
dysfunction.
A

Galantamine,
rivastigmine,
donepezil

25
Q 
Irreversible AChE
Long lasting
Insecticides
Parathion, malathion
Nerve agents
Sarin, soman
tabun, VX
Novichok Agents
A

ORGANOPHOSPHATES

26
Q

Once a bond between an organophosphate and Serine site on acetylcholinesterase is ______, it is permanently out of commission/destroyed

A

Aged

27
Q

What are the muscarinic symptoms of cholinergic toxicity?

Sludge Dumbbels

A 
Salivation
Lacrimation
Urination
Diarrhea
GI discomfort
Emesis
Diarrhea
Urination
Miosis/muscles weak
Bronchorrhea
Bradycardia
Emesis
Lacrimation
Salivation/sweating
28
Q

What are the nicotinic symptoms of cholinergic toxicity?

MTWTF

A 
Muscle cramps
Tachycardia
Weakness
Twitching
Fasciculations
29
Q

(Drug treating cholinergic toxicity)

• REGENERATES ACHE; must be given before aging

A

PRALIDOXIME (2-PAM)

30
Q

(Drug treating cholinergic toxicity)
– REQUIRES HUGE AMOUNTS
• MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT
NICOTINIC SX (PARALYSIS)

A

ATROPINE

31
Q 
•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
A

ANTICHOLINERGICS

32
Q 
(anticholinergics)
\_\_\_\_\_ AMINES HAVE CENTRAL EFFECTS
• ATROPINE, SCOPOLAMINE (SCOPACE®), 
BENZTROPINE (COGENTIN®), DICYCLOMINE 
(BENTYL®)
A

TERTIARY Amines

33
Q 
(anticholinergics)
• \_\_\_\_ amines– PERIPHERAL 
EFFECTS
• GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM 
(SPIRIVA®)
A

QUATERNARY AMINES

34
Q
  • 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
A

ATROPINE

35
Q

Where does atropine work as far as muscarinic receptor?

A

Blocks M2

36
Q 
•FOUND IN HYOSCYAMUS NIGER 
(HENBANE)
•TERTIARY AMINE
•PRIMARY USE
• MOTION SICKNESS
• VOODOO ZOMBIFICATION
A

SCOPOLAMINE

37
Q 
• QUATERNARY AMINE, FEWER 
CENTRAL EFFECTS
• USED TO DRY SECRETIONS
• SURGERY
• KETAMINE TREATMENT
• ADJUNCT FOR REVERSAL OF 
NEUROMUSCULAR BLOCKERS
- Doesn't mess with HR
A

GLYCOPYRROLATE

38
Q

______ 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)

A

ANTICHOLINERGIC

USES

39
Q

_____ 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

A

ANTICHOLINERGIC EFFECTS

40
Q

How many mg of nicotine is fatal?

A

40 mg (1 drop of pure liquid)

41
Q

(NICOTINIC DRUGS_

• PARTIAL 
AGONIST/ANTAGONIST
• LONG T½ AND HIGH AFFINITY FOR NACH(OS)
• INHIBITS:
• NICOTINE BINDING
• WITHDRAWAL SYMPTOMS
• DOPAMINE RELEASE
A

•VARENICLINE (CHANTIX®)

42
Q 
The following drugs are used as \_\_\_\_\_\_\_
• DEPOLARIZING
SUCCINYLCHOLINE
• NONDEPOLARIZING
ROCURONIUM
A

Neuromuscular blockers

43
Q 
• 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
A

SUCCINYLCHOLINE

44
Q
  • NONDEPOLARIZING
  • ONSET ~60 SECONDS
  • DURATION ~ 45 MINUTES
  • 0.6 – 1.2 MG/KG
  • NO SIGNIFICANT ADR
  • REVERSAL AGENT
A

ROCURONIUM

Pharmacology (12 decks)

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