Pharm - Nose/Oroph. Flashcards
List the 6 medications to treat AR
- Intranasal glucocorticoids (INGC)
- Antihistamines
- Decongestants
- Ipratropium bromide (Atrovent)
- Montelukast (Singulair)
- Cromolyn Sodium (Nasalcrom)
what is the most effective, single therapy for pt with persistent nasal sx associated with AR?
INGC
INGC MoA
- Inhibit allergic inflammation in the nose at many levels - Downregulate inflammatory response by binding to intracellular glucocorticoid receptors in the cell’s cytoplasm - Enter the cell’s nucleus, bind with genes, make mRNA for anti-inflammatory proteins AND suppress transcription of most cytokine and chemokine genes (produce inflammation)
INGC indication
- Moderate to severe intermittent and persistent AR - AR preferred agent, more effective than the other classes of medications
INGC contraindication
hypersensitivity to the drug
INGC ADE
- Nasal burning, stinging, dryness (related to alcohol or propylene glycol) - Nose bleeds:
INGC nose bleeds - two types
- Frank epistaxis: mechanical trauma from repeat sprays 2. Scant blood in nasal mucous: pause treatment for a few days, ensure pt using correct technique
INGC expected clinical effects
Decrease in nasal congestion, rhinorrhea, itching, sneezing
Two major types of INGC
First and second generations
What are two first generation INGC - generic - brand - dose
- Triamcinolone (Nasacrod Allergy 24) 2 sprays daily
- Budesonide nasal spray (Rhinocort) 1 spray daily
List 5 second generation INGC - generic - brand - dose
- Mometasone (Nasonex) 1 spray daily
- Ciclesonide (Omnaris) aqueous suspension pump spray 2 sprays daily
- Ciclesonide (Zetonna) pressurized aerosol spray 1 spray daily
- Fluticasone (Flonase Allergy relief, GoodSense Nasoflow) adult 2 sprays daily children 1 spray daily
- Fluticasone furoate (Flonase Sensimist): adults 2 sprays daily children 1 spray daily
Antihistamine MoA
- Bind to and activate histamine H1 and H2 (in the gut) receptors
- Compete with histamine for H1 receptors on cells (competitive antagonist) and inhibit the effects of histamine
how should antihistamines be used for best effect
regular use before/during allergen exposure to ensure med reaches all cell receptors before histamine does
What do histamines cause
vasodilation muscle constriction endothelial permeability
What are hx of histamine allergy sx
- sneezing - rhinitis - rhinorrhea - erythema - pruritus - urticaria
Antihistamine indication
- Most effective for treating nasal itching, conjunctival itching, tearing, sneezing, rhinorrhea in the nose. - Do not relieve nasal congestion
Antihistamine contraindication
- Doses should be reduced in renal and hepatic function impairment - Loratidine: use every other day in kidney or liver impairment
Antihistamine ADE 1st Gen
- CNS symptoms (sedation and impaired thinking)
- impaired driving
- HA, drowsiness, dry mouth, fatigue
Antihistamine 1st Gen ADE children
- Impaired school performance
- Paradoxical agitation <2 (can cause death)
Antihistamine 1st Gen ADE Elderly
- Anticholinergic properties: Dry mouth constipation urinary hesitance dry eyes
- Confusion: dementia-like symptoms
- Sedation
Antihistamine ADE nasal sprays
bitter taste HA sleepiness nasal burning pharyngitis
Antihistamine dosing diff between 1st and 2nd gen
1st - short half life so multiple daily doses 2nd
- longer half life so dose 1-2 daily
Antihistamine 2nd gen ADE
less sedating than 1st gen
Two 2nd gen oral antihistamines generic and brand
- Loratadine (Claritin)
- Cetirizine (Zyrtec)
Two 2nd gen nasal spray antihistamines generic and brand
- Azelastine
- Olopatadine (Patanase)
Combo product - 2nd gen antihistamine generic and brand
Azelastine & Fluticasone (Dymista)
Loratadine dose
10 mg daily =>2 yo
Decongestant MoA
- Sympathomimetics (similar to NE and epinephrine)
- Directly stimulate alpha-adrenergic receptors
- Cause vasoconstriction
Decongestant Indication
Nasal congestion
Decongestant Contraindication
- Don’t take pseudoephedrine while taking MAO inhibitor therapy or for 2 weeks after stopping MAOI
- Do not administer ER pseudoephedrine to <12
- Avoid in pts with uncontrolled HTN
Decongestants not indicated as what?
- mono-therapy for chronic AR
- most commonly used in combo with antihistamines
Oral Decongestant ADE
- CNS stimulation (nervousness, restlessness, insomnia, termor, dizziness, headache, anorexia)
- Can counteract drowsiness caused by antihistamines, tachycardia, palpitations
Nasal Decongestant ADE
- Burning
- Stinging
- Dryness
- Tolerance and rebound congestion (rhinitis medicamentosa) if used for > 1 week
Expected clinical effect decongestants
Relief of nasal congestion:
- Decreased tissue hyperemia,
- Decreased tissue edema,
- Decreased nasal congestion
- Increased nasal airway patency
One oral decongestants generic brand
Pseudoephedrine (Sudafed)
What is often being used instead of pseudoephedrine?
phenylephrine - but not as effective in the treatment of allergic rhinitis symptoms
Due to pseudoephedrine use in meth labs
One nasal spray decongestant example
Oxymetazoline (Afrin)
Ipratropium bromide (Atrovent) MoA
- Antimuscarinic agent
- Inhibits parasympathetic neurons that control secretion
Ipratropium bromide (Atrovent) Indication
Decreases rhinorrhea associated with persistent AR
Ipratropium bromide (Atrovent) Contraindication
Hypersensitivity to the drug
Ipratropium bromide (Atrovent) ADE
Dryness nose bleeds nasal irritation
Ipratropium bromide (Atrovent) Expected Clinical Effet
- Decrease rhinorrhea
- Less effective than INGC for sneezing, pruritis, nasal obstruction due to AR
Montelukast (Singulair) MoA
Blocks leukotriene 1 receptor (competitive antagonist) to decrease inflammation
Montelukast (Singulair) Indication
- Seasonal and persistent AR
- Not a first line option
- Pts who don’t tolerate or who refuse nasal sprays
Montelukast (Singulair) Contraindication
Hypersensitivity to drug
Montelukast (Singulair) ADE
- HA, abdom pain, cough, flu-like sx
- DO NOT RX to people with active, preexisting anxiety, depression or symptoms of a psych disorder
- Abnormal dreams, insomnia, anxiety, worsening depression, suicidal thinking, rare cases of suicide
Montelukast (Singulair) Expected clinical effect
- Similar efficiacy to antihistamines
- Less effective than INGC
Cromolyn Sodium (Nasalcrom) MoA
Mast cell stabilizer
– inhibits release of histamine and other inflammatory mediators
Cromolyn Sodium (Nasalcrom) Indication
- Seasonal and persistent AR
- Good for episodic symptoms to allergens (animal dander)
Cromolyn Sodium (Nasalcrom) Contraindicatino
hypersensitivity to drug
Cromolyn Sodium (Nasalcrom) ADE
- Sneezing
- nasal irritation
- unpleasant taste Very safe
Cromolyn Sodium (Nasalcrom) Expected clinical effect
- Nasal: prevent symptoms even when used within 30 min of allergic exposure
- Less effective than INGC or 2nd gen antihistamines
Non pharmaceutic way to control allergic rhinitis
nasal saline irrigation
- use alone or with other topical meds
- can be used before other topicals to clear nasal mucosa
- always use “safe” water to avoid amoebas :(
How often can nasal irrigation be used?
PRN Daily BID
Intermittent allergic rhinitis
- symptoms are present <4 days/week
- Persist for less than four weeks
Persistent allergic rhinitis
- Present >4 days/week
- Persist for more than four weeks
Mild allergic rhinitis
NO
- Sleep disturbance
- Impairment of daily activities
- Impairment of school/work
- Troublesome sx
moderate-severe allergic rhinitis
One or more of the following:
- Sleep disturbance
- Impairment of daily activities
- Impairment of school/work
- Troublesome sx
What is (maybe) the most important way to control allergic rhinitis?
environmental trigger control
what is the goal of medical treatment of AR
control symptoms while allowing usual daily activities, min ADE
Treatment of mild AR - generally start with what?
start local, move systemic
Treatment of mild AR - best option for adults - best option for children
- adult: nasal spray steroid
- child: antihistamine
Treatment of mild AR best way to use therapies?
All therapies work best when taken regularly but for very mild symptoms or intermittent exposure to known allergen, PRN use is ok
Treatment of mild AR - most effective treatment
INGC ≥ 2 years
Treatment of mild AR - how can INGC be dosed?
regularly or PRN
Treatment of mild AR - three examples of INGC to use
- mometasone - fluticasone - triamcinolone
Treatment of mild AR - when to use 2nd gen oral antihistamine
- allergen exposure can be predicted - use 2-5 hours prior to exposure
Treatment of mild AR - two 2nd gen oral antihistamines that can be easily used by children
- cetirizine - loratadine come in syrups
Treatment of mild AR - what med is best used 4-7 days prior to allergen exposure
Intranasal Cromolyn - often preferred for young children due to safety profile
Treatment of moderate-severe AR - most effective & best initial therapy
INGC - 2nd gen, low bioavailability options
Treatment of moderate-severe AR - two INGC to use
- Mometasone furcate - fluticasone furoate
Treatment of moderate-severe AR - what do if INGC fails to adequately control sx?
add a second therapy in conjunction with INGC
Treatment of moderate-severe AR - if already using INGC but still have breakthrough sx
antihistamine intranasal spray ex: azelastine + fluticasone (Dymista) for >12
Treatment of moderate-severe AR - if already using INGC but still have nasal congestion
decongestant nasal sprays (oxymetazoline) + 2nd gen oral antihistamine
Treatment of moderate-severe AR - if already using INGC but still have itching, sneezing, rhinorrhea
2nd gen oral antihistamine - cetirizine or loratadine
Treatment of moderate-severe AR - if already using INGC but still have rhinorrhea
ipratropium
Treatment of moderate-severe AR - if already using INGC but have asthma
montelukast
Treatment of moderate-severe AR - if already using INGC but still have allergic rhinitis and allergic conjunctivitis
antihistamine eyedrops
Treatment of AR in pregnant women
- Allergen avoidance - Cromolyn 2nd gen INGC (lowest effective dose) - Oral 2nd gen antihistamines: Loratadine and certirizine
what should pregnant women avoid using for AR
Oral decongestants
Treatment of AR in breastfeeding
- Allergen avoidance - Nasal saline - INGC (budesonide) or cromolyn plus cetirizine or loratadine
What are the four classes used to treat mild/intermittent AR for people >2
- oral 2nd gen antihistamines 2. Antihistamine nasal spray 3. INGC 4. Mast cell stabilizer
Oral 2nd gen antihistamine example and age it is appropriate for
Cetirizine ≥6 months
Antihistamine nasal spray example and age it is appropriate for
Aselastine (Aster) ≥5 years
INGC examples (2) and age
Mometasone furoate (Nasonex) ≥ 2 years Fluticasone furoate (Flonase) no age specified
Mast cell stabilizer and age appropriate for
Cromolyn (NasalCrom) ≥ 2 years
Most common orgs cause acute sinusitis
Gram pos: Strep pneumoniae Gram neg: H. influenza M. Catarrhalis The cat hangs out in the box again with the flu and strep
Adult abx of choice for acute sinusitis - standard dose - high dose
Standard: Augmentin due to high prevalence of beta-lactamase production by common bacteria High: Higher dose augmentin
Adult abx of choice for acute sinusitis - allergy to pen
Doxycycline levofloxacin moxifloxacin
Child abx of choice for acute sinusitis - standard
Standard: Amoxicillin
Child abx of choice for acute sinusitis - High dose (2)
2 X dose amox if high rate of s. pneumonia resistance
2X dose Augmentin if
- severe illness
- Purulent nasal discharge
- <2 yo
- Daycare attendee
- Has had abx in last 30 days
Abx of choice for acute sinusitis and NPO
IM ceftriaxone
Abx of choice for acute sinusitis with type 1 pen allergy
- Clindamycin + cefixime
- Linezolid + cefixime
- Levofloxacin
Abx of choice for acute sinusitis with non type 1 pen allergy
cephalosporins
Adjunct therapy for acute sinusitis
- Pain or fever: acetaminophen or NSAID
- INGC to reduce inflammation in nose and sinus (Risk of oral candidiasis)
what is not recommended as an adjunct therapy for acute sinusitis
Antihistamines and decongestants due to SA
Child with acute sinusitis, run through changes if unresponsive to given therapy
- 3 day observation period is ok if otherwise healthy, mild, not worsening
- 72 hours no improvement: amox +/- clavulanate
- 72 hours no improvement: high dose augmenting
- 72 hours no improvement: Clindamycin + cefixime, linezolid + cefixime, levofloxacin
What kind of observation period is considered for adults with acute sinusitis?
7 days
First line treatment for adults acute sinusitis
augmentin
when consider high dose abx for adult
- recent abx
- recent hospitalization
- >65
- immunocompromised
Tx goals in chronic sinusitis
- control of mucosal inflammation and edema
- maintenance of adequate sinus ventilation and drainage
- tx of colonizing or infecting microorganisms, if present
- reduction in the number of acute exacerbations
Most common organisms in chronic sinusitis
-aerobic:
*gram +: strep pneumoniae
*gram -: H. flu and M. cat
-anaerobic:
*if risk for MRSA, coverage for this should be included
When selecting abx therapy for adults with CRS without nasal polyposis, empirical therapy is used based on what?
- likelihood of pathogens
- hx of drug allergies
- risk factors for beta-lactamase producing organisms and MRSA
- cost
Example regimen in CRS without nasal polyposis
- amoxicillin-clavulanate for 3-4 weeks
- if penicillin allergy and MRSA suspected: clindamycin
What is the main side effect of clavulanate?
diarrhea
Abx treatment in adult with CRS with nasal polyposis
-if bacterial infection is suspected or confirmed, same abx strategy as CRS without NP
What is the most appropriate glucocorticoid tx regiment for adults w/ CRS with AND without NP?
-oral prednisone - 10 days
Maintenance therapy of CRS without NP
- intranasal glucocorticoid spray for inflam. 2. intranasal saline spray 3. tx underlying allergic rhinitis if present -allergen avoidance/immunotherapy -oral/topical antihistamine 3. antileukotriene agents in pts w/ refractory nasal congestion and PND 4. avoid chronic use of oral decongestants
Maintenance of therapy of CRS with NP
- use of topical glucocorticoids (intranasal) 2. antileukotrienes may be beneficial as adjunct 3. antihistamines can be tried in pts w/ persistent nasal symptoms despite steroid use
MoA of nystatin
binds to sterols in fungal cell membrane, changing the cell wall permeability which allows the intracellular contents to leak out. It is not absorbed through the mucous membranes or intact skin
MoA of Azole derivatives (clotrimazole, miconazole, fluconazole)
interferes w/ fungal cytochrome P450 activity, decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting cell membrane formation
Azole drug adverse effects
-GI upset -prolonged administration can cause hepatotoxicity -periodic monitoring of aminotransferases is prudent w/ chronic administration
Tx of oral candidiasis in immunocompetent infants
nystatin susp
Tx of oral candidiasis in neonates
nystatin susp
Tx of oral candidiasis in infants 30 days or older
Nystatin susp 100,000 units to each cheek (200,000 units per dose) 4 times daily for 7-14 days
Tx of oral candidiasis in children
Nystatin suspension 400,000 – 600,000 units “swish and swallow” 4 times per day for 7-14 days
Alternative tx of oral candidiasis in children
-nystatin lozenges -clotrimazole lozenges
Tx of oral candidiasis in adults that are HIV seronegative
-clotrimazole troches (low adherence d/t dose) -miconazole - effective but more expensive -nystatin - not always palatable
If there is no response to the local tx of oral candidiasis in adults, what tx is recommended?
-oral fluconazole
drug to treat oral candidiasis refractory to nystatin or other first line therapy in infants
oral fluconazole and appropriate decontamination measures of pacifiers and bottle nipples
drug to treat oral candidiasis refractory to nystatin or other first line therapy in children
oral fluconazole
Describe the role of docosanol in the treatment of mild oral herpes simplex (OHS)
-10% cream available OTC -may decrease healing time and reduce severity of symptoms when applied at the first sign of recurrence -applied 5 times per day until the lesion is healed, but for no more than 10 days
possible adverse effects of docosanol
rash and itching at site of application
role of oral and IV antiviral medications in more serious OHS infections
-may stop viral replications in the skin, but does not eliminate HSV form the body to prevent later outbreaks -Ex: valacyclovir, famciclovir, acyclovir
role of antiviral creams in more serious OHS infections
-may shorten attacks of recurrent HSV-1 if applied early, usually before lesions develop -ex: acyclovir and penciclovir cream
What is the cause of the majority of pharyngeal infections?
viruses
Common viruses that cause pharyngitis
-Adenovirus -Influenza -Parainfluenza -Rhinovirus -RSV
Most common bacterial cause of pharyngitis
group A strep (GAS)
What are some rare organisms to cause pharyngitis?
-corynebacterium diphtheriae -neisseria gonorrhoeae
Abx for pharyngitis are only indicated for what?
GAS pharyngitis
Abx of choice for GAS pharyngitis
-penicillin and amoxicillin (narrow spectrum, low incidence of ADE, low cost) Ex: penicillin VK tabs
What abx for GAS pharyngitis is preferred in pts unlikely to comply w/ 10 day course of tx?
benzathine penicillin G
What is significant about amoxicillin as tx for GAS pharyngitis?
it is the only indication for which once daily amoxicillin is acceptable
second line abx of choice for GAS pharyngitis in non type 1 penicillin allergy
1st generation cephalosporins -Cephalexin -Cefadroxil
second line abx of choice for GAS pharyngitis in type 1 penicillin allergy
-Clindamycin -Clarithromycin -Azithromycin
reason for not using aspirin in people =< 21 years old
Risk of Reye’s syndrome - a neuro complication d/t viral infection
What INGC preferred in children
second generation INGC due to low bioavailability and once daily dosing
Optimal dosing for INGC
Start with max dose for age
once symptoms are controlled, decrease dose to lowest effective dose
** diff than most drugs
How to administer INGC
Shake
Prime
Blow
Aim
Breathe and Spray
what are third generation antihistamines
active metabolites of second-gen drugs
improved clinical efficacy and min side effects
what is a good “bridge” option to use while INGC take effect
Antihistamine nasal sprays
- rapid onset (<15 min)
- can be used on demand
How to administer oral antihistamines
regularly or PRN 2-5 hours before exposure
Dosing variations for INGC
- PRN or regularly
- if can predict exposure, use 2 days before, through, and 2 days after exposure
Dosing Dosing variations for Mast cell stabilizer
- PRN or regularly
- Less effective than INGC or 2nd gen antihistamines
- QID dosing
- can use 30 min prior to brief exposure (pet dander)
- can be started 4-7 days prior to prolonged exposure