Drugs for Treatment of Ear, Eye, Nose, & Throat Problems Flashcards
Decongestants overview
alpha-adrenergic agonists
cause vasoconstriction, reduce edema
available as nasal spray or oral tablets
can act on imidazaline receptros
alpha adrenergic agonists drug list
Pseudoephedrine
prescription, or behind the counter restrictions
Phenylephrine
Naphazoline
Oxymetazoline
Tetrahydrozoline (used for eyes to get red out)
Xylometazoline
alpha adrenergic agonists overview
Effective only for relief of nasal congestion and not sneezing, itching, or discharge
Often given in combination with an H1-antihistamine
alpha adrenergic agonists
AE
Adverse effects include insomnia, excitability, headache, nervousness, palpitations, tachycardia, arrhythmia, hypertension, nausea, vomiting, and urinary retention.
Should not be used more than 3 days in order to avoid rebound congestion and rhinitis medicamentosa (drug induced rebound congestion)
Antitussives
Opioids
central suppression of cough reflex
Codeine
Dextromethorphan
Antitussives
non-Opioids
Benoxinate -local anesthetic
Diphenhydramine -antihistamine
Expectorants
overview
used in copd
Facilitate secretion or decrease viscosity of mucus to facilitate clearance of mucus secretions in airways.
N-acetyl-cysteine*
Expectorants
breaks sulfhydryl bonds in mucus proteins; makes mucus less sticky
Guaifenesin*
Expectorants
claimed to facilitate removal of viscous mucus.
Potassium iodide:
Expectorants
claimed to decrease viscosity of mucus.
Recombinant DNAse (Dornase alpha)
Expectorants
-useful in cystic fibrosis.
Other Therapy for Rhinitis
Ipratropium bromide
vasomotor rhinitis
Intranasal cromolyn sodium, nedocromil
Intranasal corticosteroids
Intranasal corticosteroids
beclomethasone dipropionate (Beconase AQ) budesonide (Rhinocort Aqua) flunisolide (generic, Nasarel) fluticasone propionate (Flonase) mometasone furoate (Nasonex) triamcinolone acetonide (Nasacort AQ)
Allergic Rhinitis
Drugs delivered locally as nasal spray
Antihistamines Antimuscarinics Cromolyn compounds Topical corticosteroids Nasal decongestants Sympathomimetic Agents -adrenergic agonists
Antihistamines:H1 Receptor Antagonists
Several structural classes
Pharmacokinetics rapidly absorbed large Vd 2nd generation drugs do not cross BBB metabolized in the liver t1/2 most drugs = 4-6 hours sustained release preparations t1/2= 12-24 hrs
What drugs act on the cholinergic muscarinic receptor
Diphenhydramine
clemastine
promethazine
they have a sedative effect in brain
what drugs act on the alpha drenergic recetpros
promthezine
what receptors act at serotonin receptors
cyproheptadine
Clinical Indications oh H1 antagonists
Acute and Chronic Allergic Rhinitis
Vasomotor rhinitis
antimuscarinic effects help
Eosinophilic nonallergic rhinitis
Viral Upper Respiratory Infection
antimuscarinic effects help
Urticaria
Allergic conjunctivitis
Anaphylactic reactions
adjunct to epinephrine
Motion sickness and nausea
Insomnia
Key Drugs -1st Generation H1 antagonists
- Diphenhydramine (Benadryl)
- Chlorpheniramine (Chlor-Trimeton)
Others Dimenhydrinate (Dramamine) Cyclizine (Marezine) Hydroxyzine (Atarax) Meclizine (Bonine) *Promethazine (Phenergan)
Key Drugs -2nd generation H1 antagonists
Cetirizine (Zyrtec) Fexofenadine (Allegra) Loratadine (generic, Claritin, Alavert) Desloratadine (Clarinex)
Azelastine (Astelin) Intranasal spray
Key Points -2nd generation H1 antagonists
Less complete distribution to CNS
little drug crosses BBB –therefore, much less sedation compared to 1st generation drugs
Have longer elimination t1/2 than 1stgeneration
therefore, longer duration of action
Lower incidence of antimuscarinic side effects, e.g. dry mouth, dysuria, etc.
Clinical Effects
antihistamines
All antihistamines are effective for relieving:
sneezing
nasal itching
nasal discharge (rhinorrhea)
Not very effective for relieving:
congestion
add decongestant
Side Effects
1stgeneration agents
h1 antagonists
sleepiness
interfere with learning
decrease work productivity
impair psychomotor performance
increases risk of injury
Patient may be unaware of these effects
Side effects may persist morning after taking drug at bedtime
Side Effects
1stgeneration agents
Sedation
antimuscarinic effect
1stgeneration only
Side Effects
1stgeneration agents
CNS
dizziness, tinnitus, nervousness, insomnia, fatigue, blurred vision
1stgeneration only
Side Effects
1stgeneration agents
GI
nausea, vomiting, loss of appetite
Side Effects
1stgeneration agents
Dry mouth
–(antimuscarinic effect)
1stgeneration only
Side Effects
1stgeneration agents
urinary retention
(antimuscarinic effect)1stgeneration only
Other Therapy for Rhinitis
Ipratropium bromide
vasomotor rhinitis
Intranasal cromolyn sodium, nedocromil
Intranasal corticosteroids beclomethasone dipropionate budesonide flunisolide fluticasone propionate triamcinolone acetonide
Antimuscarinics: Ipratropium bromide
A quaternary muscarinic receptor antagonist
Ipratropium bromide If given parenterally
effects are like atropine
Ipratropium bromide if given as an aerosol
treat COPD
few side effects, even when swallowed because is poorly absorbed from GI and does not cross into brain
quaternary amine-poor diffusion across membranes
Ipratropium bromide parasympathetic
mediated bronchospasm is a significant component of airway resistance in some asthmatics and COPD patients, especially psychogenic exacerbations
Ipratropium bromide
Therapeutic Use:
Bronchodilation develops more slowly and is usually less intense than that produced by -agonists.
Useful bronchodilation lasts up to 6 hours.
Principal use of ipratropium is in COPD.
Combined with albuterol = COMBIVENT
*Also used intranasally (Roxane) to reduce secretions in the upper and lower respiratory tract in allergic rhinitisand chronic postnasal drip syndrome.
Cromolyn Compounds
drugs
Cromolyn sodium nasal spray (Nasalcrom)
Cromolyn sodium (Intal)
Cromolyn Compounds
Cromolyn compounds are *anti-inflammatoryagents that indirectly inhibit antigen-induced bronchospasm and directly inhibit the release of histamine and other autocoids from sensitized mast cells.
May suppress the activating effects of chemoattractant peptides on eosinophils, neutrophils, and monocytes.
Cromolyn Compounds:Therapeutic Use
Cromolyn compounds *do not directly relax smooth muscle, therefore they are not useful for control of acute bronchospasm.
Cromolyn compounds are primarily *prophylactic. When inhaled several times daily, they inhibit both the immediate and late asthmatic responses to antigenic challenge or exercise.
Used mostly in mild to moderate asthma as an added therapy or as a prophylactic alternative to inhaled steroids or oral methylxanthines.
cromolyn compounds
adverse effects
are infrequent and generally mild
Intranasal Corticosteroids
overview
*Most effective drugsavailable for relief of symptoms of allergic rhinitis
Available in aqueous solution/pump spray formulations
They all reduce sneezing, itching, discharge, and congestion
Most are effective when given once daily
Take at least one week to be maximally effective.
Intranasal Corticosteroids
Side Effects –usually mild
Dryness & irritation or burning of nasal mucosa
Sore throat
Epistaxis
Headache
Leukotriene Modifier overview
Montelukast(Singulair)
Cysteinyl leukotrienes (cousins of prostaglandins) released in nasal mucosa during allergic inflammation.
Oral montelukast blocks leukotriene receptor
Modestly beneficial for relief of sneezing, itching, discharge, and congestion
Safe and with few side effects
Leukotriene Modifier
One study showed montelukast to be as effective
as loratadine, but not as effective, alone or in combination with loratadine, as an intranasal corticosteroid
Allergic Conjunctivitis
overview
The most common form of ocular allergy
Usually associated with allergic rhinitis
May be seasonal or perennial
Main symptom is itching
Allergic Conjunctivitis
Treatment
Oral antihistamines (2ndgeneration) usually effective
Topical antihistamine eye drops
also effective
may be more rapid acting
also antiinflammatory
Allergic Conjunctivitis
*Antihistamine/decongestant combinations
pheniramine/naphazoline (Visine A)
antazoline/naphazoline (Vasocon-A)
Available over-the-countermay be more effective than either agent alone but are short actingand can cause rebound vasodilation with continued use
Topical Ocular H1 -Antihistamines
Azelastine (Optivar)
Emedastine difumarate (Emadine)
Levocabastine HCl (Livostin)
Topical Ocular Mast Cell Stabilizers
Cromolyn sodium (generic, Crolom)
Lodoxamide tromethamine (Alomide)
Nedocromil sodium (Alocril)
Pemirolast potassium (Alamast)
H1 Antihistamine+ Mast Cell Stabilizers
Ketotifen fumarate (Zaditor)
Olopatadine HCl (Patanol)
These drugs are primarily antihistamines but are marketed as also having mast cell stabilizing activity. Probably all H1 antihistamines have mast cell stabilizing activity.
Antiviral Agents
*Amantadine& Rimantadine
RNA viruses
Inhibit uncoating of viral nucleic acids
Inhibit viral replication
*Prophylaxis of type A influenza
Treatment initiated within 48 hours after initial appearance of symptoms is effective
Oseltamivir (*Tamiflu), oral
Inhibits neuraminidase of influenza A or B
Hemagglutinin on viral surface binds to host cell receptors allows virus entry
Neuraminidase on viral surface sugar from receptor. This step required for release of progeny viral particles
Also inhibits viral spread
*Bird flu = H5N1 strain
Zanamivir (*Relenza)
same as Tamiflu but with an inhaler
side effects of antihistamine are just
if taken chronically and at high doses
tetrhydrozoline
visine
Ipratropium bromide blockes
muscarinic decreases secretion so used for nasal drip
A quaternary muscarinic receptor antagonist
permanently charged doesnt cross membranes
young kids dont want to put on
steroids
Intranasal corticosteroids control
symptoms then stop taking
antihistamines Molecular Mechanism of Action
slow hours at the soonest
steroids
heat shock proteins
turning on and off packets of genes
glucocorticoids summary of action
inhibits migration and activation of cells in immune resposne
poor wound healing
Inhibits neuraminidase of influenza A or B
prevents entry into cell