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Pharmacology > PNS Drugs > Flashcards

PNS Drugs Flashcards

1
Q

Carbachol

A
  • muscarinic agonist, non-specific with significant nicotinic activity
  • not susceptible to AChE activity
  • used to obtain miosis after surgery and for reducing IOP in 24 hrs after cataract surgery
  • adverse reactions: Iritis or corneal clouding
  • precautions: Acute cardiac failure, bradycardia, asthma, peptic ulcer, urinary tract obstruction, Parkinsonism
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2
Q

Methacholine

A
  • muscarinic agonist with slight nicotinic activity
  • Used in diagnosis of airway hyperreactivity
  • adverse reactions: Headache, throat irritation, lightheadedness, itching
  • precautions: Acute cardiac failure, bradycardia, asthma, peptic ulcer, urinary tract obstruction, hyperthyroidism
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3
Q

Bethanechol

A
  • Muscarinic agonist, no nicotinic activity
  • DOC for promoting GI and urinary motility for post-op and post-partum non-obstructive urinary retention/ neurogenic atony of urinary bladder/ post-op gastric atony or gastroparesis
  • precautions: Acute cardiac failure, bradycardia, asthma, peptic ulcer, urinary tract obstruction, hyperthyroidism, Parkinsonism
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4
Q

Pilocarpine

A
  • Muscarinic agonist, plant alkaloid optained from pilocarpus microphyllus. Higly active on salivary and sweat glands in addition to eyes
  • Contracts ciliary and circular muscles, producing miosis, increases outlfow of aqueous humor
  • Treatment of open- or closed- angle glaucoma, miosis allowing for outflow of aqueous humor, treatment of xerostomia caused by Sjogren’s
  • adverse reactions: Blurred vision (accomodation), hypersalivation, diaphoresis, flusing, headache
  • contraindications: Asthma, iritis, retinal detachment, adhesion between iris and lens
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5
Q

Nicotine

A
  • nicotinic agonist, used to help smokers quit
  • Agonist at NM and NN receptors with complex CNS and PNS action. Stimulates catecholamine release from adrenal medulla
  • precautions: Angina, arrhythmia, MI, hypertension, pheochromocytoma, diabetes, vasospastic disease, thyroid disease, Pregnancy D for transdermal/ C for other routes
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6
Q

Varenicline

A
  • nicotinic agonist
  • 1 week ramp up before quitting smoking, taken while quitting smoking to reduce cravings and reward from smoking
  • High affinity partial agonist at a4B2 receptors, moderate affinity at 5-HT3 receptors
  • Minimal metabolism, 92% excreted unchanged in urine. T1/2 about 24 hours
  • adverse events: GI issues common. Insominia and neuropsychiatric symptoms- black box warning (hostility, agitation, depression, suicidal thoughts)
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7
Q

Physostigmine

A
  • carbamoyl class acetylcholinesterase inhibitor. Competes with ACh for its binding site on acetylcholinesterase, ↑ ACh. Actions mimic cholinergic stimulation
  • DOC to counteract toxic anticholinergic effects of other drugs and second line treatment of glaucoma
  • precautions: Heart disease, hyperthyroidism, peptic ulcer
  • contraindications: Asthma, GI obstruction, ileus, urinary tract obstruction
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8
Q

Neostigmine

A
  • carbamoyl ester class acetylcholinesterase inhibitor; mimics cholinergic stimulation
  • similar to physostigmine but cannot cross BBB so peripheral effects only. 2-4 hour duration of action
  • treatment of myasthenia gravis, post-op removal of neuromuscular blockade, ileus
  • same precautions/ contraindications as physostigmine
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9
Q

Edrophonium

A
  • alcohol class acetylcholine inhibitor
  • used for dx of myasthenia gravis- very short duration of action so not good option treatment
  • precautions: heart disease, asthma
  • contraindications: GI obstruction, ileus, urinary tract obstruction
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10
Q

Ecothiophate

A
  • organophosphate class acetylcholinesterase inhibitor by phosphorylation
  • second line treatment for closed angle glaucoma
  • adverse effects: Eye: stinging, blurred vision, lacrimation, increased incidence of cataracts with prolonged therapy
  • precautions: uveitis
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11
Q

Pralidoxime

A
  • Reverses AChE inhibition by organophosphates if given within 24 hours of exposure, reactivates AChE by displacing phosphoryl group from AChE that has been modified/ inhibited
  • precautions: Renal insufficiency, AChE inhibitor tx for myasthenia gravis
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12
Q

Atropine

A
  • competitive muscarinic receptor antagonist used to treat bradycardia and as pre-op agent to reduce secretions, mydriatic agent for opthalmic exams
  • metabolized by liver
  • precautions: Chronic pulmonary disease, thickens mucus, conditions that increase core body temperature (exercise, fever)- blocks sweat
  • contraindications: Acute MI, bladder obstruction, prostatic hypertrophy, glaucoma, GI obstruction, ileus, hyperthyroidism
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13
Q

Oxybutynin

A
  • competitive muscarinic receptor antagonist used as a bladder muscle relaxant to treat incontinence. Less activity than atropine but more anti-spasmodic activity than atropine
  • metabolized by CYP3A4
  • adverse effects: CNS: dizziness, confusion, headache, drowsiness, CV: palpitations, tachycardia, GI: constipation, diarrhea- depending on individual predominant tone
  • contraindications: GI obstruction, ileus, urinary tract obstruction, urinary retention, toxic megacolon, ulcerative colitis, uncontrolled narrow-angle glaucoma
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14
Q

Ipratropium

A
  • Muscarinic receptor antagonist, blocks Ach effect on bronchial smooth muscle
  • TX for acute asthma episode, first line treatment in COPD with persistent symptoms
  • does not cross BBB well
  • precautions: Glaucoma, urinary retention
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15
Q

Mecamylamine

A
  • Competitive antagonist at nicotinic NN receptors
  • Overall effect depends on predominant ANS tone at target
  • Used to treat hypertension that does not respond to other agents; used experimentally in Tourette’s and nicotine withdrawal
  • Administered PO, almost completely absorbed and excreted unchanged in urine
  • side effects:CNS: choreiform movements, mental changes, paresthesias, seizures, dizziness; CV: postural hypotension, tachycardia; GI: xerostomia, constipation, ileus; UG: urinary retention, impotence; Eye: blurred vision, mydriasis
  • precautions: Cerebral or coronary atherosclerosis or other conditions of deficient blood flow; Recent MI; Glaucoma; Renal insufficiency
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16
Q

Epinephrine

A

-Mixed-acting agonist, activates both a and b receptors throughout the body
- TX for acute bronchospasm asthma, CPR; DOC for anaphylaxis; in open angle glaucoma decreases IOP and causes brief mydriasis Administered IV or by inhalation/ topically to eye, poor PO bioavailability. Metabolized by COMT and MAO
- side effects: CNS: anxiety, nervousness, insomnia, aggressive behavior; CV: arrhythmias, PVCs, tachycardia
Precautions: Narrow-angle glaucoma, Intraarterial administration, Nonanaphylactic shock, Labor, Extravasation, Hypertension, Hyperthyroidism, Diabetes
- often used to complement local anesthetics- prolong duration of action and maintain local effects

17
Q

Phenylephrine

A
  • selective a1 agonist- no significant B effects at therapeutic doses
  • used to treat nasal congestion- local application causes vasoconstriction–> decreased mucus secretion. used as a diagnostic aid in opthamology- causes transient mydriasis
  • metabolized by MAO but NOT COMT
  • few adverse reactions. parenteral route can cause angina, hypertension, anxiety, insomnia
  • precautions: CV disease, narrow angle glaucoma, labor, hyperthyroidism
18
Q

Clonidine

A

-Agonist at presynaptic a2 receptors (autoreceptors), results in inhibition of sympathetic outflow and tone → decreased sympathetic tone reduces HR, TPR, MAP, CO, and SV
- Used mainly in the TX of hypertension, has been used ADHD, opioid and nicotine withdrawal, vascular headaches, cancer pain, and Tourette’s syndrome. Hypotensive effect is mainly due to actions on the brainstem. Epidural admin. produces analgesia that is not blocked by opiod antagonists
- PO bioavailability approaches 100%, Highly lipid soluble, distributes widely throughout the tissues, including the CNS
- side effects: CNS: sedation (33-50%), lethargy, dizziness (10%); CV: orthostatic hypotension (3%), palpitations, tachycardia, bradycardia
GI: xerostomia (some salivation regulated by a receptors) (40-50%), NV, constipation
precautions: Abrupt DC → withdrawal syndrome consisting of rebound in catecholamines → severe hypertension, tachycardia, agitation; Breast-feeding;
CV disease: MI, or severe heart failure- may decrease perfusion and worsen ischemia in these conditions

19
Q

Isoproterenol

A

-potent agonist at b1 and b2 adrenergic receptors, with little or no effect on a receptors
- Norepinephrine analog used to improve AV conduction during heart block and as cardiac stimulant in cardiac arrest- causes increase in CO and decrease in vascular resistance; used in acute bronchospasm, asthma, COPD- Metabolism mainly by COMT but bad substrate for MAO
side effects: CNS: nervousness, headache. CV: palpitations, tachycardia, angina; flushed skin
- precautions: Arrhythmias, heart block caused by digitalis compounds, coronary artery disease, coronary insufficiency, diabetes, hyperthyroidism

20
Q

Dobutamine

A
  • primarily an agonist at b1 adrenergic receptors, with minor b2 and a1 effects
  • used to treat acute heart failure. Clinical effect= increased myocardial contractility and stroke volume with increased CO
  • Give by IV only, rapid onset, short half life, metabolism by COMT and glucuronidation, give only for a few days
    side effects: CV: PVCs, tachycardia, angina
    precautions: Idiopathic hypertrophic subaortic stenois, arrhythmia, hypovolemia
21
Q

Salmeterol

A
  • B2 agonist, stimulates B2 receptors in lung to cause relaxation and bronchodilation
  • used as long-term prophylactic treatment of asthma, bronchospasm, COPD.
  • onset takes 14 min.- do not use for acute asthma attack. Admin by oral inhalation, effects for 12 hours, excretion in feces. Large bulky alkyl structure- long half life at receptor
  • side effects: cough, headache, pharyngitis, upper respiratory tract infection
  • precautions: Coronary artery disease, hypertension, hyperthyroidism, diabetes
    FDA black box warning of increased risk of asthma related death with use of long acting B2 agonists
22
Q

Phentolamine

A
  • Competitive antagonist at a1 and a2 receptors, can block 5-HT receptors and release histamine at larger concentrations
  • clinical effect of a antagonism is inhibiton of vasoconstriciton and decrease in blood pressure. used to prevent hypertensive episodes during surgery for pheochromocytoma; used to prevent dermal necrosis following extravasation of alpha agonists
  • Administered IV for BP control pre-op and SC for necrosis. Short half life (19 min)
  • side effects: CNS: dizziness; CV: orthostatic hypotension, reflex tachycardia, arrhythmias
    GI: NVD; Nasal congestion (a1 agonists used for decongestion)
  • precautions: MI, coronary insufficiency, angina
23
Q

Phenoxybenzamine

A
  • noncompetitive selective a1 antagonist with very minor a2 activity. Forms a stable covalent bond with receptors
  • clinical effects= vasodilation, inhibition of adrenergically medicated sweating, reflex tachycardia. Used for tx of sweating and hypertension in pheochromocytoma, may use to tx urinary symptoms of BPH, and for vasospastic conditions- Raynaud’s, frostbite low oral bioavailability, extensive distribution because highly lipophilic, clinical effects for 7 days after stopping therapy
  • side effects: CNS: dizziness, syncope, fatigue
    CV: reflex tachycardia, orthostatic hypotension; UG: impotence; Eye: miosis; Nasal congestion
  • precautions: Congestive heart failure, coronary artery disease, renal disease: hypotensive effects can worsen these conditions
24
Q

Prazosin

A
  • competitive antagonist at a1 receptors; causes peripheral vasodilation, lower vascular resistance, lowers BP
  • used in treatment of hypertension; used off-label to treat BPH (many a1 receptors on urinary sphincter- blocking causes relaxation of sphincter and greater urination)
  • Some delay in reaching therapeutic anti-hypertensive effects.
  • side effects: CNS: dizziness (first-dose syncope), lightheadedness, drowsiness, headache; CV: palpitations, orthostatic hypotension; GI: pain, NVD; GU: impotence, incontinence
  • precautions: Angina; prazosin-induced hypotension may worsen condition
    Syncope can be hazardous for patients in occupations for which alertness is required
    Caution with PDE5 inhibitors- Viagra, etc. vasodilation effects are enhanced
25
Q

Tamsulosin

A
  • Competitive antagonist at postsynaptic a1 receptors; 10X selective for a1A receptors vs. a1B receptors; ~70% of a1 receptors in prostate are a1A subtype
  • Preferred drug for treatment of BPH (many a1 receptors on urinary sphincter- blocking causes relaxation of sphincter and greater urination) Long acting, effects are not highly dose-dependent. Food decreases bioavailability.
  • Metabolized by CYP3A4 and CYP2D6
  • side effects: CNS: dizziness, insomnia, syncope; CV: orthostatic hypotension; GU: abnormal ejaculation (8%);
  • precautions: Take on empty stomach. Caution with PDE5 inhibitors
26
Q

Yohimbine

A
  • antagonist at presynaptic a1 autoreceptors, increase in noradrenergic nerve activity, increased sympathetic tone
  • used in tx of ED- increased blood flow to penis
27
Q

Propranolol

A
  • competitive, non-selective antagonist of B receptors. Decrease HR at rest and on exertion, decrease in systolic and diastolic BP, decreased skeletal muscle perfusion
  • TX for hypertension, angina, acute MI, prophylaxis of MI, prophylaxis of migraine/ anxiety/ agitation/ panic attack - B blockade decreases somatic symptoms of anxiety causing improvement in psycologic components as well
  • Widely distributed because lipophilic, extensively metabolized on first pass
  • side effects: CNS, CV:bradycardia, cold hands and feet; GI: NVD
  • side effects: Hepatic disease; Raynaud’s disease; Diabetes (
  • precautions: Abrupt DC can produce myocardial ischemia, MI, arrhythmias, or severe hypertension; Acute bronchospasm, pulmonary edema, asthma; Bradycardia, AV block
28
Q

Timolol

A
  • Competitive, non- selective B adrenergic antagonist. Reduces IOP by reducing aqueous humor production
  • First line tx for open angle glaucoma opthalmic solution delivered to eye, little systemic absorption. Metabolized in liver, excreted from kidney
  • side effects: eye pain, conjunctivitis, itching, dizziness, headahce
  • precautions: hepatic disease, Raynaud’s, diabetes
  • contraindications: acute bronchospasm, pulmonary edema, asthma, bradycardia, AV block
29
Q

Metoprolol

A
  • Competitive b1-selective adrenergic receptor antagonist
  • Effect is ↓ in both resting and exercise HR and CO, and ↓ in both systolic and diastolic BP
  • TX of angina, hypertension, migraine headaches, MI,heart failure, and tremor
  • side effects: CNS: depression, dizziness, fatigue; CV: bradycardia, AV block, hypotension, cold hands and feet; GI: xerostomia, NVD
  • precautions: hepatic disease, Raynaud’s, diabetes
  • contraindications: Abrupt DC can produce myocardial ischemia, MI, arrhythmias, or severe hypertension; Acute bronchospasm, pulmonary edema, asthma; Bradycardia (< 45 BPM), AV block
30
Q

Pindolol

A
  • Non-selective B partial agonist with intrinsic sympathomimetic activity, in presence of full agonist causes attenuation of sympathetic tone;
    Also partial agonist at 5-HT1A receptors and may augment anxiolytic effects of SSRIs
  • good when mainteneance of adequate sympathetic tone is desirable.
  • Used in tx for hypertension, heart failure, heart block, bronchospasm. Augments SSRI action for anxiet
  • side effects: CNS: dizziness, fatigue. CV: edema
    precautions; diabetes
  • contraindications: Abrupt DC can produce myocardial ischemia, MI, arrhythmias, or severe hypertension
31
Q

a-methyltyrosine

A
  • Blocks tyrosine hydroxylase which catalyzes the first step in catecholamine biosynthesis, decreased catecholamine activity
  • Causes decreased frequency and severity of hypertensive attacks. Used pre-op for removal of pheochromocytoma or for chronic treatment of pheochromocytoma
  • side effects: CNS: usually transient sedation, anxiety, depression, hallucinations, disorientation, confusion, speech difficulty, drooling, tremor. GI: diarrhea (10%); Crystalluria with doses > 2 g QD. do not take with alcohol (sedative effect)
32
Q

a-methyldopa

A
  • prodrug converted in-vivo to a-methylnorepinephrine (a false neurotransmitter). Acts on a2 autoreceptors in brainstem to decrease NE release, sympathetic tone, baroreceptor response
  • Used as tx for hypertension, DOC during pregnancy. Used in tx of pheochromocytoma, pre-op and chronic treatment
  • side effects: CNS: transient sedation, parkinsonism, elevated LFTs, hemolytic anemia
  • precautions: Hepatic disease, dopamine antagonists
33
Q

Reserpine

A
  • Inhibits vesicular neurotransmitter storage, causes long-lasting depletion of 5-HT, NE, and DA in CNS and periphery leading to decrease in peripheral vascular resistance, decreased BP, bradycardia; CO, renal blood flow, and glomerular filtration rate are also decreased
  • first anti-hypertensive drug discovered but less commonly used now due to newer drugs that are equally effective and better tolerated
  • Readily absorbed but latency until anti-hypertensive effects are noticed, then anti-hypertensive effects persist for weeks after stopping therapy
  • side effects: many, including severe depression. let to monoamine hypothesis of depression
34
Q

Botulinum toxin

A
  • Zinc proteinase: cleaves SNAP-25, a synaptic protein required for vesicle fusion with axon terminal → ↓ ACh release
  • indicated for facial wrinkles, axillary hyperhydrosis, cervical dystonia, strabismus, blepharospasm
35
Q

Amphetamine

A
  • Indirect-acting sympathomimetic: inhibits NE, DA, and 5-HT uptake transporters; also evokes monoamine release via reverse transport (causes efflux of cytosolic monomamines but does NOT depolarize neuron)
  • Used for ADHD or narcolepsy and off label for obesity (causes anorexia)
36
Q

Cocaine

A
  • Reversibly decreases nerve permeability to Na+, inhibiting electrical conduction
    Inhibits neuronal transporters for uptake of 5-HT, E, NE, and DA
  • Used as topical anesthetic and vasoconstrictor for short ENT procedures. Produces local vasoconstriction, which facilitates examination and surgery by ↓ congestion, swelling, and bleeding at the site of application
    CNS effects are euphoria, stimulation, ↓ fatigue, sexual stimulation, ↑ alertness
37
Q

Paroxetine

A
  • Highest specificity for 5-HT uptake transporters of all SSRIs. Has slight anticholinergic activity
  • Used in the TX of major depression, all major anxiety syndromes, OCD, post-traumatic stress disorder, off-label uses include premature ejaculation and hot flashes
  • Latency in onset of action
  • side effects: CNS: drowsiness, dizziness, insomnia, anxiety, anorexia; GI: NV (25%), xerostomia (18%), constipation
  • precautions: renal insufficiency, hepatic disease, pregnancy category D
  • contraindications: if taking MAOIs
38
Q

Atomoxetine

A
  • norepinephrine reuptake inhibitor, no appreciable 5-HT or DA transporter affinity or affinity for other receptor sites
  • First nonstimulant drug for ADHD, FDA approved 2002
  • side effects: CNS: fatigue, emotional lability, insomnia, headache, restlessness, decreased libido; CV: chest pain, tachycardia, hypertension
    GI: upper GI pain, NV, anorexia, constipation
    UG: problems with ejaculation, urinary hesitation
  • precautions: Hepatic disease, jaundice; Narrow-angle glaucoma; taking MAOIs; CV: CVD, CAD, HTN, stroke, tachycardia, arrhythmias; pulse and BP should be monitored at baseline, after any dose increases, and periodically throughout treatment
    Black box warning for increased suicidal ideation
39
Q

Phenelzine

A
  • Non-selective, irreversible inhibitory of MAO-A and MAO-B; causes increase in concentration of NE, 5-HT, and DA
  • Second-line TX for depression for patients who are unresponsive to newer medications
    Effective in refractory anxiety disorders, OCD, social anxiety disorder, panic disorder
  • Plasma half life unrelated to duration of enzyme inhibition (irreversible enzyme inhibitor). Latency in onset
  • side effects: Sympathomimetic effects: hypertension, agitation, insomnia, tachycardia, mydriasis, diaphoresis, tremor, aggressiveness
  • must avoid tyramine-containing foods

Pharmacology (7 decks)

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