Unit 4

PSNS

cholinergic receptors located in the smooth muscle, cardiac muscle, and glands

SNS

cholinergic receptors located in the heart, blood vessels, skeletal muscle

parasympathetic nervous system

what system do cholinergic drugs stimulate?

indirect-acting anticholinesterase drugs

MOA: reversible inhibition of cholinesterase in the brain → increases Ach

TEs: mild-moderate Alzheimer’s disease

AEs: N/V/D/A, bradycardia, fainting, falls, fall-related fx, worsened PUD, urinary obstruction, bronchospasm

• donepezil (Aricept)

• galantamine (Razadyne)

• rivastigmine (Exelon)

cholinergic crisis

result of overstimulation of cholinergic & nicotinic receptors

early signs abd cramps, salivation, flushing, N/V, pinpoint pupils, transient syncope, transient complete heart block, dyspnea, ortho hypotension

late signs: circulatory collapse, respiratory arrest, hypotension, bloody diarrhea, shock, cardiac arrest

tx: atropine

Salivation Lacrimation Urinary incontinence Diarrhea GI cramps Emesis

what is the SLUDGE acronym to remember signs of cholinergic crisis?

NMDA antagonist

helps cells from burning out from too much glutamate

TEs: moderate-severe Alzheimer’s disease

AEs: dizziness, headache, confusion, constipation

• memantine (Namenda)

psychosis

syndrome of neurocognitive symptoms that impairs cognitive capacity leading to deficits of perception, functioning, and social relatedness

hallmark sign: loss of contact w/ reality

ex: schizophrenia, depressive disorders, etc.

neuroleptic malignant syndrome (NMS)

potentially life threatening condition

signs: high fever, unstable BP, myoglobinemia

extrapyramidal symptoms (EPS)

adverse effect of antipsychotics

signs: muscle sx similar to Parkinson’s, akathisia, acute dystonia

tx: benztropine, trihexyphenidyl

tardive dyskinesia

adverse effect of antipsychotics

signs: involuntary contractions of oral & facial muscles, choreoathetosis

occurs with long-term use

metabolic syndrome

adverse effect of antipsychotics

signs: insulin resistance, weight gain, changes in serum lipid levels, agranulocytosis & hemolytic anemia

increased SI

adverse effect of antipsychotics in children & young adults

increased muscle movements

adverse effect of antipsychotics in pregnant patients

increased risk of death

adverse effect of antipsychotics in elderly adults

haloperidol (Haldol)

MOA: unknown, competitively blocks dopamine receptors

uses: long-term tx of psychosis, acute/severe psychosis

contraindications: Parkinson’s, w/ CNS depressants

routes: PO, IM, IV

atypical antipsychotics

MOA: block specific dopamine receptors (D2)

• clozapine (Clozaril)

• risperidone (Risperdal)

anxiolytics

benzodiazepines & atypical anxiolytics (buspirone) are drug classes in what category?

antidepressants

SSRIs, SSNRIs, tricyclic, & MAOIs are drug classes in what category?

benzodiazepines

MOA: depress activity in brainstem & limbic system

uses: ETOH withdrawal, insomnia, muscle spasms, adjunct for depression

AEs: habit forming & high abuse potential, CNS depression, hypotension, N/V/C, resp depression

• alprazolam (Xanax)

• diazepam (Valium)

• lorazepam (Ativan)

-lam/-pam endings

buspirone

non-sedating, non-habit forming anxiolytic

contras: do not administer w/ MAOIs or SSRIs (→ serotonin system)

AEs: paradoxical anxiety, blurred vision, headache, nausea (take with food)

interactions: grapefruit juice, St. John’s wort, MAOIs

flumazenil

what drug is used for overdose of benzodiazepines?

antidepressants

which drug category has several drugs with black box warnings d/t increase in suicidal ideation in patients?

SSRIs

MOA: selectively inhibits serotonin reuptake

TEs: slight CNS excitation (may → insomnia)

AEs: withdrawal syndrome, sexual dysfunction, EPS sx, wt gain, postural hypotension, serotonin syndrome, SI

interactions: MAOIs, antiplatelet/anticoagulants, TCAs, lithium

• fluoxetine

• sertraline

• citalopram

• escitalopram

SSNRIs

MOA: block serotonin & norepinephrine reuptake

AEs: dizziness, drowsiness, headache, GI upset, anorexia, hepatotoxicity

interactions: SSRIs, triptans, alcohol

• venlafaxine

• duloxetine

serotonin syndrome

begins 2-72 hours after tx or OD of serotonin drug

• myoclonus, incoordination, hyperreflexia, excessive sweating, tremor, tachycardia, fever

resolves spontaneously after d/c drug

tricyclic antidepressants (TCAs)

MOA: block reuptake of serotonin, norepinephrine, and possibly epinephrine

uses: depression, childhood enuresis, OCD, adjunct for chronic pain, appetite stimulant for anorexia

contras: recent MI, pregnancy

AEs: sedation, impotence, ortho hypotension, anticholinergic effects

overdose: very lethal!! (→ death d/t seizures or dysrhythmias)

• amitriptyline (Elavil)

monoamine oxidase inhibitors (MAOIs)

MOA: converts norepinephrine, serotonin, and dopamine → inactive products

interactions: tyramine (→ HTN crisis)

• phenelzine

most hazardous!!