PHARMA 2 Flashcards
CLASS: Adrenergic antagonist (alpha 1- selective)
MOA: Selectively blocks alpha-1 adrenergic receptors
INDICATION:
● Benign prostatic hyperplasia
● Hypertension
SIDE EFFECT:
First dose orthostatic hypotension
Reflex tachycardia
PRAZOSIN
CLASS: Adrenergic antagonist (beta non - selective)
MOA: Blocks β1 and β2 receptors. Blocks sympathetic effects on heart and BP
INDICATION:
● Angina prophylaxis
● Hypertension
● Arrhythmias
● Migraine
● Performance
anxiety
● Hyperthyroidism
SIDE EFFECTS:
● Bronchospasm
● AV block
● Heart failure
● CNS sedation
● Erectile
dysfunction
May mask symptoms of hypoglycemia in diabetic
PROPRANOLOL
CLASS: Adrenergic antagonist (beta 1 - selective)
MOA: Selectively blocks β1 receptors. Blocks sympathetic effects on heart and BP
INDICATION:
● Angina
● Hypertension
● Heart failure
SIDE EFFECTS:
● Bronchospasm
(less common)
● AV block
● Heart failure
● CNS sedation,
erectile dysfunction
ATENOLOL
NURSING INTERVENTION FOR ADRENOCEPTORS BLOCKERS
● Monitor VS (esp BP and HR)
● Report any complaint of stuffy nose
● For clients with DM, have glucagon available and follow adjustment of insulin dose as ordered
● Not to stop abruptly the medication
● Slowly rise from supine or sitting to standing position
● Primary transmitter in all autonomic ganglia and at the synapses between parasympathetic postganglionic
neurons and their effector cells
● Primary transmitter at the somatic (voluntary) skeletal muscle neuromuscular junction
ACETYLCHOLINE
● Not very useful for systemic therapy because their effects are not sufficiently selective
○ Parasympathetic and sympathetic ganglia and somatic neuromuscular junctions all may be blocked
● Botulinum toxin is a very large molecule and diffuses very slowly
○ Injection for relatively selective local effects
CHOLINERGIC DRUG EFFECTS
M1 -
M2 -
M3 -
Nn -
Nm -
LOCATIONS:
M1 - NERVE ENDINGS
M2 - HEART, SOME NERVE ENDINGS
M3 - EFFECTOR CELLS, SMOOTH GLANDS
Nn - ANS GANGLIA
Nm - NEUROMUSCULAR END PLATE
DIRECT ACTING:
MUSCARINIC -
CHOLINE ESTERS -
ALKALOIDS -
NICOTINIC -
INDIRECT ACTING:
MUSCARINIC - EDROPHONIUM (SHORT ACTING)
CHOLINE ESTERS - CARBAMATES (INTERMEDIATE TO LONG-ACTING)
ALKALOIDS - ORGANOPHOSPHATES (VERY LONG-ACTING)
NICOTINIC -
DIRECT ACTING CHOLINOMIMETIC:
CLASS: Cholinomimetic (direct - acting, muscarinic)
MOA: Activates M3 receptors in ciliary muscle
INDICATION:
● Glaucoma
● Sjögren syndrome — Xerostomia
SIDE EFFECTS:
● Miosis
● Blurring of vision
PILOCARPINE
DIRECT ACTING CHOLINOMIMETIC:
CLASS: Cholinomimetic (direct - acting, muscarinic)
MOA: Activates muscarinic (M1-M3) receptors. Act on M receptors only
INDICATION: Bladder and Bowel atony
SIDE EFFECT:
● Cyclospasm
● Diarrhea
● Urinary urgency
● Vasodilation
● Reflex
tachycardia
● Sweating
BETHANECHOL
DIRECT ACTING CHOLINOMIMETIC:
CLASS: Cholinomimetic (direct - acting, muscarinic)
MOA: Activates nicotinic Ach receptors
INDICATION:
● Smoking cessation
SIDE EFFECTS:
● Generalized ganglionic stimulation
NICOTINE
● CNS stimulation
● Eye: Miosis, spasm of accommodation
● Lungs: Bronchoconstriction
● GIT/GUT: Excessive gastrointestinal and
genitourinary smooth muscle activity
Muscarinic Toxicity
● Bind to cholinesterase and undergo prompt hydrolysis
○ Alcohol portion released
○ Acidic portion retained and released slowly
- Prevents the binding and hydrolysis of endogenous acetylcholine
INDIRECT ACTING CHOLINOMIMETICS
● Ganglionic stimulation
● Blockade of neuromuscular end plate
depolarization
Nicotinic Toxicity
INDIRECT ACTING CHOLINOMIMETIC:
CLASS: Cholinomimetic (indirect - acting)
MOA: Inhibits acetylcholinesterase, amplifies endogenously released acetylcholine
INDICATION:
● Myasthenia gravis (diagnosis - Tensilon test)
SIDE EFFECT:
● Miosis
● Salivation
● Nausea
● Vomiting
● Diarrhea
● Bradycardia
NEOSTIGMINE
INDIRECT ACTING CHOLINOMIMETIC:
CLASS: Cholinomimetic (indirect - acting, muscarinic)
MOA: Inhibits acetylcholinesterase, amplifies endogenously released acetylcholine
INDICATION:
● Myasthenia gravis (diagnosis - Tensilon test)
SIDE EFFECT:
● Miosis
● Salivation
● Nausea
● Vomiting
● Diarrhea
● Bradycardia
EDROPHONIUM
Acute worsening of symptoms due to infection,
stress or under medication
Myasthenic Crisis Cholinergic Crisis
INDIRECT ACTING CHOLINOMIMETIC:
CLASS: Prototype nonselective muscarinic blocker
MOA:
Found in Atropa belladonna
Tertiary amine that readily crosses membrane barriers
INDICATION:
● Mydriatic
● Cycloplegic
● Antidote for organophosphate
● Bradycardia
● Hypersalivation
SIDE EFFECTS:
● Tachycardia
● Mydriasis
● Cycloplegia
● Skin flushing
● Delirium
● Hallucinations
ATROPINE
● Autoimmune destruction of nicotinic Ach receptors characterized by:
○ Fluctuating muscle weakness
○ Ocular symptoms
○ Bulbar symptoms
○ Proximal muscle weakness
Myasthenia Gravis
● Excessive activation of cholinoreceptors (skeletal
muscle weakness and parasympathetic signs) due to
overmedication
Myasthenic Crisis Cholinergic Crisis
● Malathion and Parathion: Insecticide
● Sarin, Tabun, Soman: Nerve gasses
● Signs and symptoms: (DUMBBELSS)
○ Diarrhea
○ Urination
○ Miosis
○ Bronchospasm
○ Bradycardia
○ Excitation
○ Lacrimation
○ Sweating
○ Salivation
● Antidote: Pralidoxime (ASAP, Not >36 Hours)
Nursing Consideration/s:
● WOF for bronchospasms, wheezing, bradycardia
● Rise slowly from supine or sitting position to avoid
dizziness or fall
● Monitor VS
ORGANOPHOSPHATE POISONING
How does edrophonium differentiate myasthenic crisis from cholinergic crisis?
● improves muscle strength in myasthenic crisis
● weakens muscle strength in cholinergic crisis
● Side effects:
○ Atropine fever (Hyperthermia)
○ Atropine flush (cutaneous vasodilation)
○ Mydriasis and cycloplegia (paralysis of ciliary
muscles = loss of accommodation)
○ Decreased secretions (saliva, sweat,
bronchiolar)
○ Tachycardia
○ Arrhythmias (Intraventricular conduction blocks)
○ Constipation
○ Blurred vision
○ CNS toxicity
● Antidote: Physostigmine
MNEMONIC FOR ATROPINE TOXICITY:
1. Hot as hare (Increased Temperature)
2. Dry as a bone (Thirsty, decreased secretions)
3. Red as Beet (Flushed Face)
4. Blind as Bat (Blurred Vision)
5. Mad as Hatter (Confusion, delirium)
ATROPINE TOXICITY
Contraindication to Muscarinic Blockers:
● Cautious use in infants
○ Hyperthermia due to decreased sweating
● Acute angle-closure glaucoma
● Benign Prostatic Hyperplasia