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1.1 Pharmacology-OMS2 > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

what receptor predominates in the heart

A

M2

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2
Q

Which neuronal pathways are specific to the sympathetic nervous system?

Specify the neurotransmitters and receptor types?

A

Sympathetic

Neurotransmitters: NE > Epi (DA); ACh

Receptors: α, β, (D), nAChR, mAChR

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3
Q

which neuronal pathways are unique to the parasympathetic nervous system?

which neurotransmiters?

which receptors?

A
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4
Q

Location, structural features, & MOA for M1 receptors

A

M1

Nerves

GPCR, Gq/11

IP3, DAG cascade

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5
Q

Location, structural features, & MOA for M2 receptors

A

M2

  • Heart, nerves, smooth muscle
  • GPCR, Gi/o
  • Inhibition of cAMP production, activation of K+ channels
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6
Q

Location, structural features, & MOA for M3 receptors

A

M3

Glands, smooth muscle,endothelium

GPCR, Gq/11

IP3, DAG cascade

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7
Q

Location, structural features, & MOA for M4 receptors

A

M4

CNS

GPCR, Gi/o

Inhibition of cAMP production

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8
Q

Location, structural features, & MOA for M5 receptors

A

M5

CNS

GPCR, Gq/11

IP3, DAG cascade

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9
Q

Location, structural features, & MOA for NN receptors

A

NN

Postganglionic cell body, dendrites, CNS

α and β only

Examples: (α4)2(β4)3; (α7)5

Na+, K+ depolarizing ion channel

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10
Q

which receptors are predominate in smooth muscle?

A

M3, M2

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11
Q

predominate receptors in the eye

A

M3, M2

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12
Q

predominate receptors in the heart

A
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13
Q

predominate receptors in endothelium

A

M3

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14
Q

predominate receptors in glands

A

M3, M2

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15
Q

predominate receptors in the lungs

A

M3, M2

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16
Q

predominate receptors in GI/GU tracts

A

M3, M2

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17
Q

predominate receptors in CNS

A

M1-M5

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18
Q

role of cholinergic agonists

identify the subtypes and MOAs

A

mimic actions of ACh on nAChRs and mAChRs

Direct acting: directly stimulate muscarinic or nicotinic receptors

indirect acting: influence enzymes that then exert an effect on ACh

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19
Q

MOA for direct acting cholinergic agents

Identify 4 direct agonists

A
  • MOA: agonists at cholinergic receptors
  • Metabolized by acetylcholinesterase
  1. Acetylcholine
  2. Methacholine
  3. Carbachol
  4. Bethanechol
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20
Q

3 groups of AChE inhibitors

identify chemical traits of each

A

1) Alcohols
- reversible
- charged
- poorly absorbed
2) Carbamic acid esters
- reversible but longer lasting than alcohols
- charged
- poorly absorbed
3) Organophosphates
- irreversible (covalent)
- uncharged
- HIGHLY absorbed

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21
Q

what happens to eyes with direct parasympathetic stimulation?

A

Eye

Sphincter muscle of iris = Contraction (miosis)

Ciliary muscle = Contraction for near vision

22
Q

what happens to the heart with direct parasympathetic stimulation?

A

Heart

Sinoatrial node = ↓ in rate (negative chronotropy)

Atria = ↓ in contractile strength (negative inotropy). ↓ in refractory period

AV node = ↓ in conduction velocity (negative dromotropy) & ↑ in refractory period

Ventricles = Small ↓ in contractile strength

23
Q

what happens to the BVs with direct parasympathetic stimulation?

A

Blood vessels

Arteries = Dilation (via EDRF). Constriction (high-dose direct effect)

Veins = Dilation (via EDRF). Constriction (high-dose direct effect)

24
Q

direct parasympathetic effect on the lungs

A

Lung

Bronchial muscle= Contraction (bronchoconstriction)

Bronchial glands = Stimulation

25
Q

Direct parasympathetic effects on GI tract

A

Gastrointestinal tract

  • Motility = Increase
  • Sphincters = Relaxation
  • Secretion = Stimulation
26
Q

Direct parasympathetic effects on th GU tract

A

Urinary bladder

Detrusor = Contraction

Trigone and sphincter = Relaxation

27
Q

Eye disorders treated using direct-acting cholinergic agonists

A

Diseases of the eye

  • Glaucoma
  • Accommodative esotropia: misalignment of the eyes caused by hypermetropic accomodative error
28
Q

Primary pharmacological agent used to treat GI/GU disorders: GI/GU disorders

  • Postoperative ileus
  • Congenital megacolon
  • Urinary retention
  • Esophageal reflux
  • Xerostomia d/t Sjögren syndrome
A

direct-acting cholinergic agonists

goal: stimulate parasympathetics

29
Q

If a patient presents to the ED and there’s a suspicion of cholinergic agonist toxicity, what Sx might be present to confirm the Dx?

A

SLUDGE CRITERIA

S - salivation

L- lacrimation

U- urinary frequency

D- diaphoresis/diarrhea

G-GI cramps/pain

E- emesis

  • or

DUMBBELs criteria

D- diaphoresis/diarrhea

U- urinary frequency

M - Miosis (pupil constriction)

B - Bronchospasm/bronchorrhea

E - Emesis

L - Lacrimation

S- Salivation

nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, bronchial constriction, increase in glandular secretion (SLUDGE)

30
Q

SLUDGE Criteria

A

SLUDGE CRITERIA

S - salivation

L- lacrimation

U- urinary frequency

D- diaphoresis/diarrhea

G-GI cramps/pain

E- emesis

–signs of toxicity from direct acting cholinergic agonists targing mAChRs

31
Q

DUMBBELS Criteria

A

DUMBBELS criteria

D- diaphoresis/diarrhea

U- urinary frequency

M - Miosis (pupil constriction)

B - Bronchospasm/bronchorrhea

E - Emesis

L - Lacrimation

S- Salivation

-signs of mAChR agonist toxicity

32
Q

In what situations will use of muscarinic stimulants be contraindicated?

A

Muscarinic stimulants

  • Predictable - nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, bronchial constriction, increase in glandular secretion (SLUDGE)
  • Contraindicated in patients who have asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease
33
Q

If a patient presents with nicotine toxicity, what would you predict to uncover as the source during H&P?

What Sx would concern you the most and require emergent action?

If they do have nicotinic overstimulation from a direct-acting cholinergic agonist, how will you treat them?

A

Nicotinic stimulants

  • Nicotine poisoning: from cigarettes and insecticides
  • Acute toxicity includes CNS stimulation, skeletal muscle end plate depolarization, respiratory paralysis, hypertension, cardiac arrhythmias

Tx: atropine and parenteral anticonvulsants (diazepam, a benzodiazepine)

34
Q

pt presents with dry mouth and gritty feeling eyes

Dx and Tx?

A

Dx: Sjögren syndrome

Tx with direct acting cholinergic agonists

Tx option 1: Cevimeline

•Oral tablet used to treat dry mouth (xerostomia) in patients with Sjögren syndrome

Tx option 2: Pilocarpine

•Approved for xerostomia treatment in patients with Sjögren syndrome or head and neck cancer treatment related xerostomia (PO), miosis during ophthalmic procedures (topical), and for glaucoma (topical)

Pure mAChR agoni

35
Q

Drug of choice to induce miosis during eye surgery

A

use a direct acting cholinergic agonist

Acetylcholine

Approved for intraocular use during surgey, causes miosis (reduction in pupil size)

Carbachol

•Nonspecific cholinergic agonist that is used for the treatment of glaucoma or to produce miosis during surgery or ophthalmic examination

36
Q

Indications and adverse effects for use of Bethanechol

A

Bethanechol: direct acting cholinergic agonist

  • Selective mAChR agonist that primarily affects the urinary and GU tracts
  • Tx: patients with urinary retention and heartburn
  • Pro: Little cardiovascular stimulation
  • Con: May produce urinary tract infection if sphincter fails to relax
37
Q

Indications and adverse effects for use of Verencicline

A

Varenicline (Chantix)

  • Use: FDA approved for smoking cessation
  • Partial agonist that binds with high affinity and selectivity to α4β2 nAChRs (NN)
  • MOA: stimulation and subsequent moderate, sustained release of mesolimbic dopamine are thought to reduce craving and withdrawal symptoms associated with smoking cessation
  • Side Effects: Nausea is most common adverse effect;

Serious adverse effects: neuropsychiatric sx such as behavior change, agitation, depressed mood, suicidal ideation, and attempted and completed suicide

38
Q

Most common clinical indications for use of INDIRECT acting cholinergic agonists

A

Use #1: Glaucoma

•Stimulation of mAChRs on the ciliary body facilitates aqueous humor outflow and reduces intraocular pressure (replaced by β-blockers, prostaglandins)

Use #2: Dementia (Alzheimer and Parkinson Diseases)

•Patients with Alzheimer Disease dementia have a deficiency of intact cholinergic neurons (particularly those extending from subcortical areas such as the nucleus basalis of Meynert)

Use #3: Antidote to anticholinergic poisoning

  • From atropine, antihistamines, TCAs, sleep aids, cold preparations
  • Sx – cutaneous vasodilation, anhidrosis, anhydrotic hyperthermia, nonreactive mydriasis, delirium, hallucinations, reduction/elimination of the desire to urinate

Use #4: Reversal of neuromuscular paralysis

Use #5: Myasthenia gravis

39
Q

Sx and Tx for AChE inhibitor Toxicity

A
  • AChE inhibitor toxicity
  • Sx: SLUDGE or DUMBBELS, effects on NMJ
  • Combination Tx needed:
  1. atropine (central & peripheral effects)
  2. maintenance of vital signs (respiratory is key)
  3. decontamination (remove clothing, wash skin)
  4. pralidoxime (cholinesterase regenerator)
40
Q

Contrast effects of cholinergic agonists vs cholinergic antagonists

A
41
Q

explain subgroups of cholinergic antagonists

which are most clinically useful?

A

Muscarinic and nicotinic subgroups

Antinicotinic agents

  • Neuromuscular junction (skeletal muscle relaxants)
  • Ganglia (rarely used)

Antimuscarinic agents

  • CNS, nerves, heart, smooth muscle, glands, endothelium
  • Block the effects of parasympathetic autonomic discharge

•The most clinically useful cholinergic antagonists

Prototype antimuscarinic agent: atropine

42
Q

What are the following drugs used for?

Scopolamine

A

Drugs used for motion sickness

•Scopolamine

route: PO, injection, transdermal

43
Q

What are the following drugs used for?

  • Atropine
  • Dicyclomine
  • Glycopyrrolate
  • Hyoscyamine
A

Drugs for gastrointestinal disorders (hypermobility, traveller’s diarrhea)

  • Atropine**
  • Dicyclomine
  • Glycopyrrolate
  • Hyoscyamine

Often combined w/opioid antidiarrheal drug to discourage abuse of the opioid agent

•Example: Lomotil - combination of atropine and diphenoxylate

44
Q

What are the following drugs used for?

  • Atropine
  • Cyclopentolate
  • Homatropine
  • Scopolamine
  • Tropicamide
A

Drugs used in ophthalmology

  • Atropine
  • Cyclopentolate
  • Homatropine
  • Scopolamine
  • Tropicamide

Prob: prevent synechia formation in uveitis and iritis ( iris sticks to lens or cornea)

Tx: Homatropine & atropine

  • Pros: Long-acting agents
  • Mydriasis may last 6 hours to 12 days and cycloplegia persists about 10 hours to 14 days

ONLY use mAChR antagonists when cycloplegia or prolonged mydriasis (pupil dilation) is required.

Example: Refractive eye surgery (LASIK)

Otherwise: Use α-adrenergic receptor agonists are shorter-acting and produce less adverse effects

45
Q

What are the following drugs used for?

  • Ipratropium
  • Tiotropium
A

Drugs used for respiratory disorders

  • Ipratropium: 1st line therapy for asthma
  • Tiotropium (longer acting): COPD Tx bc longer bronchodilator action

Both are inhalation mAChR antagonists (anticholinergic drugs)

side effect: dry mouth/throat

46
Q

What are the following drugs used for?

  • Darifenacin
  • Oxybutynin
  • Solifenacin
  • Tolterodine
  • Trospium
A

Drugs used for urinary disorders

•Oxybutynin

  • selective M3 antagonist
  • side effects: dry mouth/eyes (xerostomia), dizziness, constipation, blurred vision

These are M3 but have longer half-life and lower side effects

  • Darifenacin
  • Solifenacin
  • Tolterodine
  • Trospium
47
Q

What are the following drugs used for?

•Atropine (+ pralidoxime)

A

Drugs used for cholinergic poisoning

•Atropine (+ pralidoxime): must use both together!

Causes:

  1. cholinesterase inhibitor insecticides
  2. wild mushrooms
  3. chemical warfare nerve gasses
  • Antimuscarinic agents (atropine) are given to reduce mAChR stimulation
  • No effective treatment at nAChR (pralidoxime)
  • Atropine is useless in delayed-onset mushroom poisoning
  • characterized by vomiting and nausea 6-12 hrs after ingestion and causes hepatic/renal cellular injury by amatoxins that inhibit RNA polymerase
48
Q

What are the following drugs used for?

  • Benztropine
  • Biperiden
  • Orphenadrine
  • Procyclidine
  • Trihexyphenidyl
A

Drugs used for movement disorders: Parkinson’s Ds

note: not as effective as dopaminergic tx

  • Benztropine (3o amine)
  • Biperiden
  • Orphenadrine
  • Procyclidine (3o amine)
  • Trihexyphenidyl (3o amine)
49
Q

what is the general effect of anticholinergic drugs

A

increase sympathetic tone

50
Q

What effect would use anti-cholinergic drugs have on the following systems?

CNS

Eye

Cardio

Respiratory

GI

GU

Sweat Glands

A

CNS = Sedation, drowsiness, amnesia, hallucinations, tremor reduction

Eye = Pupil dilation, cycloplegia (ciliary muscle paralysis), loss of accommodation, secretion reduction

Cardio= Tachycardia

Respiratory =Bronchodilation and secretion reduction

GI tract = Reduce salivation, gastric secretion, prolonged gastric emptying time

GU tract = Urinary retention

Sweat glands = Suppression of thermoregulatory sweating by inhibiting sympathetic cholinergic nerve fibers (remember: no parasympathetic innervation of sweat glands)

51
Q

Anticholinergics: adverse effects

A

Anticholinergics adverse effects if used to reduce GI secretions

mydriasis

cycloplegia

High systemic concentrations lead to block of parasympathetic function:

dry as a bone, blind as a bat, red as a beet, mad as a hatter, hot as a hare

•Tx: AChE inhibitors or symptomatically

52
Q

Anticholinergics: contraindications

A

Anti-cholinergic Use Contraindications/caution:

don’t use in patient’s with the following:

  1. Glaucoma
  2. Prostatic hyperplasia
  3. Acid-peptic disease

1.1 Pharmacology-OMS2 (4 decks)

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