ANS and ENT Medications

Phentolamine

α1 & α2-adrenoceptor antagonists

MOA: Competitively blocks alpha-adrenergic receptors—> brief antagonism of epinephrine and norepinephrine to reduce hypertension and minimizes tissue injury

Indications: Extravasation of norepinephrine, hypertensive crisis

Side effects: bradycardia, hypertension, tachycardia, pruritis of skin, diarrhea, upper abdominal pain, vomiting

Prazosin (minipress)

α1-adrenoceptor antagonist

MOA: Competitive inhibition of post-synpatic alpha adrenergic receptors—> vasodilation of veins and arterioles—> lower blood pressure

Indications: hypertension

Side effects: intraoperative floppy iris syndrome (IFIS): higher surgical complication rates

Tamsulosin (Flomax)

α1A-adrenoceptor antagonist

MOA: Antagonist of alpha1A adrenoreceptors in the prostate resulting in smooth muscle relaxation in the bladder and prostate

Indications: benign prostatic hyperplasia

Side effects: intraoperative floppy iris syndrome (IFIS): higher surgical complication rates, orthostatic hypotension

Propranolol (Inderal)

ß1 & ß2 antagonist

MOA: Non selective beta-adrenergic blocker (class II antiarrhythmic), competitively blocks response to beta 1 and beta2 adrenergic stimulation, reduces portal pressure by producing splanchnic vasoconstriction (beta 2 effect) thereby reducing portal blood flow

Indications: angina, cardiac arrhythmias, hypertension, migraine headache prevention, MI, pheochromocytoma, hypertrophic cardiomyopathy, off label: performance anxiety disorder

Side effects: bradyarrhythmias, second-degree atrioventricular block, complete atrioventricular block, bronchospasm, CNS effects: fatigue, insomnia, vivid dreams, memory impairment, sexual disorder, potentiation/masking of hypoglycemia, withdrawal (tachycardia, hypertension, exacerbation of angina pectoris, acute myocardial infarction)

Metoprolol (Lopressor, Toprol XL)

ß1> ß2 antagonist

MOA: Selective inhibitor of beta1 adrenergic receptors, competitively blocks beta1 receptors with little or no effect on beta2 receptors at oral doses <100mg (in adults)

Indications: HFrEF= heart failure with reduced ejection fraction, hypertension, post-MI

Side effects: Bradyarrhythmias (bradycardia, sinus pause, first-degree atrioventricular (AV) block), Bronchospasm, CNS effects; Fatigue, sleep disturbance, insomnia, Potentiation/masking of hypoglycemia, Withdrawal

Carvedilol (Coreg)

ß > α1 antagonist

MOA: Nonselective beta-adrenoceptor and alpha-adrenergic blocking activity
Indications: HFrEF= heart failure with reduced ejection fraction 

Post MI left ventricular dysfunction

Side effects: Bradyarrhythmias (bradycardia, sinus pause, first-degree atrioventricular (AV) block), Bronchospasm, CNS effects; Fatigue, sleep disturbance, insomnia, hypoglycemia, Withdrawal

Betaxolol (Betoptics)

ß1 Blocker Topical

MOA: Competitively blocks beta1 receptors, with little or no effect on beta 2 receptors

Indications: Treatment of elevated intraocular pressure in patients with chronic open-angle glaucoma

Side effects: eye discomfort, altered blood pressure

Metyrosine (Demser)

Tyrosine Hydroxylase Inhibitor

MOA: Blocks the rate-limiting step in the biosynthetic pathway of catecholamines reducing their biosynthesis by 35% to 80%

Indications: Pheochromocytoma= rare tumor in adrenal glands

Side effects: CNS: extrapyrimidal reaction, GI: diarrhea

Oxymatazoline (Afrin)

Decongestant

MOA: Vasoconstriction (direct-acting alpha agonist)

Indications: Short term nasal decongestion (3-5 days maximum)

Side effects/ADRs: Rebound mucosal congestion and vascular irritation, stinging, burning, dryness, sneezing; hypertension in large dose; epistaxis, tachyphylaxis

Contraindications: continuous use, glaucoma

Dx-Dx: Alfa blockers, ergot derivatives

Monitoring: length of use

PG: not studied

Lactation: not studied

Others: bridge to nasal steroid spray; rhinitis medicamentosa management- try steroid nasal spray; doesn’t relieve itching or allergic rhinitis

Azelastine HCl (Astelin NS)

antihistamine

MOA: H1 blocker
Indications: allergic rhinitis

Side effects/ADRs: Headache, bitter taste, rhinitis, cough, somnolence; hypertension, tachycardia, anxiety, glaucoma

Contraindications: hypersensitivity, glaucoma

Dx-Dx: other anti-cholinergic or sedating drugs

Monitoring: none

PG: C

Lactation: caution

Others: Relief of sneezing, rhinorrhea and itching (mucosal) but not nasal congestion; can have systemic absorption; as an antihistamine can have anti-cholinergic impacts

Fluticasone (Flonase NS)

steroid

MOA: Anti-inflammatory with vasoconstrictor activity
Indications: Rhinitis (allergic, occupational, atrophic +/-, vasomotor +/-), nasal polyps

Side effects/ADRs: burning, irritation, epistaxis; nasal septal perforation, ulceration; bronchospasm, cough, pharyngitis

Contraindications: Hypersensitivity, recurring epistaxis, glaucoma, cataracts

Dx-Dx: none

Monitoring: epistaxis

PG: B

Lactation: administer after feeding to minimize dose given to infant

Others: minimal systemic bioavailability; very weak HPA (Hypothalamis pituitary adrenal) suppression effect; dose once to twice daily; frequently delayed impact 7-14 days

Ipratropium Bromide (Atrovent NS)

Antimuscarinic

MOA: Blocks acetylcholine at muscarinic receptors in parasympathetic nervous system
Indications: vasomotor rhinitis

Side effects/ADRs: Epistaxis, dryness, nausea; avoid with glaucoma

Contraindications: Hypersensitivity

Caution in asthma, prostatic hypertrophy, angle-closure glaucoma

Dx-Dx: other anticholinergics

Monitoring: Symptomatic improvement; side effects

PG: B

Lactation: caution

Others: Also available for inhalation (Atrovent HFA MDI)= COPD or asthma

Not very helpful for allergic symptoms but good for rhinorrhea

0.03% kids solution

0.06% adult solution

Cromolyn Sodium (Nasalcrom)

mast cell stabilizer

MOA: Stabilizes mast cell membrane so mediators (histamine, leukotrienes, etc) not released
Indications: allergic rhinitis

Side effects/ADRs: Local stinging, burning, unpleasant taste, sneezing; occasional epistaxis

Contraindications: hypersensitivity

Dx-Dx: none

Monitoring: symptom improvement; epistaxis

PG: OK in peds and pregnancy

Others: 4 times daily administration; 3-14 days delay onset,

Inhalation form for asthma and ophthalmic form for allergies, More effective in kids versus adults

Diphenhydramine (Benadryl)

Antihistamine 1st generation

MOA: H1 blockers
Indications: allergic rhinitis

Side effects/ADRs: drowsiness; anti-cholinergic side effects

Contraindications: prostatic hypertrophy, dementia (early onset due to ACh depletion), caution in asthma, close-angle glaucoma

Dx-Dx: other sedating drugs especially other anti-cholinergic drugs

Monitoring: symptoms, anticholinergic impact especially sedation

PG: unknown

Lactation: unknown

Others: not as effective as nasal corticosteroids for inflammation, kids may have excitatory impact, significant anti-cholinergic impact in elderly

Fexophenadine HCl (Allegra)

antihistamine 2nd generation

MOA: H1 receptor blocker
Indications: allergic rhinitis

Side effects/ADRs: Headache, somnolence (not as much as H1 blocker), dizziness; increases any anticholinergic effect of other co-administered drugs

Contraindications: Hypersensitivity

Caution in asthma, prostatic hypertrophy, angle-closure glaucoma, dementia

Dx-Dx: Verapamil (increases fexophenadine concentration), diminishes impact of acetylcholinesterase inhibitors in dementia

Monitoring: Symptom improvement; anticholinergic impact

PG: C

Lactation: caution

Others: Not sedating but not as effective as nasal corticosteroids; does not cross the blood brain barrier to any significant extent

Neomycin, Colistin, Hydrocortisone, Thonzonium [Cortisporin-TC]

Otic antibiotic/steroid topical

MOA: Antibacterial and anti-inflammatory
Indications: otitis externa no TM perf

Side effects/ADRs: Mucosal irritation and edema with overuse; Neomycin sensitivity can develop during course of use

Contraindications: Hypersensitivity- especially to neomycin (canal more erythema—> discontinue and use new medication)

Dx-Dx: none

Monitoring: effectiveness, ear canal edema

PG: unknown

Lactation: unknown

Others: Neomycin can be very sensitizing and create symptoms of otitis externa and rash

Cipro/Dexamethasone Otic [Ciprodex Otic]

Otic antibiotic/steroid topical

MOA: Antibacterial and anti-inflammatory
Indications: Acute otitis externa with intact tympanic membrane; AOM with vent tube

Side effects/ADRs: Mucosal irritation and edema with over use

Contraindications: Viral otic infections (herpes simplex)

Dx-Dx: none

Monitoring: symptoms

PG: C

Lactation: unknown

Others: acidic and can be painful

Nystatin (Mycostatin)

MOA: Binds to fungal membrane, creates pores in membrane disrupting membrane integrity
Indications: Thrush, oral candidiasis in immune intact host

Side effects/ADRs: Unpleasant taste, NVD; too toxic for systemic use (IV or IM)

Contraindications: hypersensitivity

Dx-Dx: none

Monitoring: effectiveness

PG: C

Lactation: caution

Others: Suspension: Swish, Swirl, Swallow 4 times daily, oral form not absorbed systemically

Meclizine (Antivert)

MOA: Anticholinergic impact on chemoreceptor trigger zone; blocks conduction in middle ear vestibular-cerebellar pathway
Indications: Prevent/treat vertigo, motion sickness

Side effects/ADRs: Sedation, thickening bronchial secretions

Contraindications: Hypersensitivity; caution in asthma, prostatic hypertrophy, angle-closure glaucoma, dementia

Dx-Dx:Avoid ethanol (increases sedation effect), other anticholinergic medications

Monitoring: effectiveness

PG: B

Lactation: unknown

Others: only “possibly effective”

Acyclovir (Zovirax)

MOA: Blocks herpes virus nucleic acid synthesis
Indications: HSV-1, HSV-2 (~1/2), VZV (~1/10), EBV (~1/10), CMV (less), HHV-6 (less); treatment and suppression

Side effects/ADRs: N, D, headache; nephritis, tremors, delirium, seizures with overdose

Contraindications: hypersensitivity

Dx-Dx: Probenicid, cimetidine increases concentration (risk neuro and renal toxicity); acyclovir decreases elimination of MTX

Monitoring: CrCl, response

PG: B

Lactation: caution

Others: Requires viral kinase so only in virus infected cells; eliminated via kidneys, oral availability is ~10-30% and decreases with increased dosing, PO chronic genital suppression herpes safe to 10 years, genital herpes patient decreased viral shedding ~90% and decreased risk of transmission ~50%

Valacyclovir= better but more money

Betaxolol (Betoptic S)

Glaucoma: beta blocker topical

MOA: Reduces IOP by decreasing production of aqueous humor
Indications: Chronic open-angle glaucoma, ocular hypertension

Side effects/ADRs: Ocular discomfort, bradycardia, bronchospasm, depression, heart block; exacerbation heart failure

Contraindications: Sinus bradycardia, Heart block > 1^st degree

Dx-Dx: Multiple potentially but minimally absorbed as ophthalmic prep

Monitoring: IOP

PG: C

Lactation: caution

Others: Benzalkonium chloride (stabilizing agent) may be absorbed by contact lens (stains them, wait 15-30 minutes before putting them in), not for sole use in angle-closure glaucoma

Half life is 12 hours, used as drug of second choice

Bimatoprost [Lumigan]

Glaucoma: prostaglandin topical

MOA: Synthetic analog of prostaglandin which decreases IOP by increasing outflow of aqueous humor
Indications: Chronic open-angle glaucoma or ocular hypertension; hypotrichosis of eyelashes (oily eyelashes with crusting)

Side effects/ADRs: Ocular hyperemia, growth of eyelashes, ocular pruritis, headache, dry eyes, photophobia, brown pigmentation or iris and eyelid with long-term use

Contraindications: <16 years old

Dx-Dx: NSAIDs decrease effect

Monitoring: IOP

PG: C

Lactation: caution

Others: Benzalkonium chloride (stabilizing agent) may be absorbed by contact lens

Half life is ~45 minutes

First line drug but expensive

Brimonidine [Alphagan P]

Glaucoma: Alpha 2 agonist topical

MOA: Selective agonism for alpha2 receptors causes reduced production of aqueous humor and increased outflow
Indications: Chronic open-angle glaucoma or ocular hypertension

Side effects/ADRs: Somnolence, allergic conjunctivitis, hyperemia, eye pruritis, hypertension, xerostomia, CNS depression

Contraindications: children <2 years old

Dx-Dx: Other CNS depressants, Beta blockers, MAO inhibitors (antidepressants)

Monitoring: IOP

PG: B

Lactation: not recommended

Others: Benzalkonium chloride (stabilizing agent) may be absorbed by contact lens

Half life is ~2 hours

Dorzolomide [Trusopt Generic]

Glaucoma: Carbonic anhydrous Inhibitor, Topical

MOA: Reversible inhibition of renal carbonic anhydrase causing increased renal excretion sodium, potassium, bicarbonate and water with decreased production of aqueous humor

Indications: Chronic open-angle glaucoma or ocular hypertension

Side effects/ADRs: Eye discomfort, superficial punctate keratitis, ocular allergic reaction, blurred vision, photophobia; possible SJS

Contraindications: History of severe Sulfa allergy, Concurrent use with oral carbonic anhydrous inhibitors

Dx-Dx: Other carbonic anhydrase inhibitors

Monitoring: IOP

PG: C

Lactation: not recommended

Others: Caution in hepatic and renal impairment; don’t use eGFR <30ml/min

Benzalkonium chloride (stabilizing agent) may be absorbed by contact lens

Half life is ~4 months

Less frequently used now

Prednisone

Corticosteroid

MOA: Inhibition of cytokines and inflammatory mediators
Indications: Short-term use in RA (multiple others)

Side effects/ADRs: Weight gain, fluid retention, straie, impaired wound healing, osteoporosis, HTN, mood changes, cataracts, hyperglycemia, dyslipidemia, peptic ulcer disease (PUD), HPA suppression, HF

Contraindications: infection, TB

Dx-Dx: live vaccines, multiple

Monitoring: CrCl, (hepatic function panel) HFP, CBC

PG: OK in pregnancy at or lower than 10mg/daily

Lactation: caution

Others: Down titrate dosing if more than 2 weeks (hypothalamus, pituitary)

Pilocarpine [Salagen]

Cholinergeic Agonist

MOA: Stimulates cholinergic receptors to increase exocrine gland function (sweat, salivary glands) and increases smooth muscle tone in GI and urinary tracts
Indications: dry mouth (xerostomia)

Side effects/ADRs: Increases toxic effects of other cholinergic agonists; flushing, dizziness, headaches, urinary frequency

Contraindications: Use with other cholinergic agonists, Asthma

Dx-Dx: See Lexicomp

Monitoring: Cardiovascular, pulmonary system impact

PG: not recommended

Lactation: unknown

Others: More fluid excretion- exacerbate heart failure and pulmonary edema