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Pharmaceutics 1
Week 3
55
Other
Graduate
01/19/2020

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Term
Intermittent Allergic Rhinitis (IAR)
Definition
Symptoms ≤ 4 days/week or ≤4 weeks
Term
Persistent Allergic Rhinitis (PER)
Definition
Symptoms >4 days/week and >4 weeks
Term
Mild severity symptoms of allergic rhinitis
Definition
Do not impair sleep or daily activities no troublesome symptoms
Term
Moderate-Severe symptoms of allergic rhinitis
Definition
Sleep disturbance, impaired daily activities (work, school)
Term
Allergic Rhinitis exclusions for self-treatment
Definition
-Children<12 years
-Pregnant or lactating women
-Non-allergic rhinitis
-Otitis media, sinusitis, bronchitis, or other infection
-Undiagnosed or uncontrolled asthma (wheezing, SOB), COPD or other lower respiratory disorder
-Severe or unacceptable side effects of treatment
Term
Non-allergic rhinitis causes
Definition
-hormonal: pregnancy, puberty, thyroid disorders
-structural: septal deviation , adenoid hypertrophy
-drug-induced: cocaine, beta-blockers, ACEIs, chlorpromazine, clonidine, reserpine, hydralazine, oral contraceptives, aspirin or other topical decongestants
-Systemic Inflammatory: eosinophilic nonallergic rhinitis (NARES)
-Lesions: nasal polyps, neoplasms
-Traumatic: recent facial or head trauma
-autonomic: age-related, physical or chemical agent causes
Term
Symptoms of allergic rhinitis
Definition
-bilateral, worst in the a.m. improve during the day, worsen in the p.m.
-frequent sneezing, paroxysmal
-sneezing anterior, watery
-variable nasal obstruction
-frequent conjunctivitis
-sinus pain due to congestion, throat pain due to postnasal drip
-anosmia: loss of sense of smell is rare
-epistaxis is rare
-facial, nasal or throat features: allergic shiners, Dennie's lines, allergic crease, allergic salute, allergic gape, non-exudative cobblestone appearance of posterior oropharynx
Term
Symptoms of non-allergic rhinitis
Definition
-unilateral common, can be bilateral, constant day/night
-little or none
-rhinorrhea: posterior, watery, thick and/or mucopurulent
-nasal obstruction is often present, often severe
-pain is variable depending on the cause
-anosmia: loss of sense of smell is frequent
-epistaxis is recurrent
-facial, nasal or throat features: nasal polyps, nasal septal deviation, enlarged tonsils and/or adenoids
Term
Treatment of allergic rhinitis
Definition
-sequential: allergen avoidance, pharmacotherapy, and allergen immunotherapy
-intranasal corticosteroids are the most effective: beclomethasone, budesonide, fluticasone, or triamcinolone
-antihistamine are commonly used, but less effective: non-sedating antihistamines are preferred over sedating based on efficacy and safety
Term
Allergen avoidance
Definition
-check local pollen counts and air quality index
-keep windows shut
-avoid yard work/outdoor sports with high pollen
-remove triggers (i.e. cats, dust mites, tobacco smoke, mold)
-lower humidity to reduce molds (ie: vent kitchen and bathrooms)
-remove house plants
-wash bedding (130F) weekly, encase mattresses and pillows in coverings resistant to dust mites
Term
Intranasal Corticosteroids (INCS)
Definition
-Budensonide (Rhinocort Allergy): >6 years
-Fluticasone (Flonase Allergy Relief): >4 years
-Triamcinolone (Nasacort Allergy 24 hour) >2 years
-may take 1 week to control symptoms
-shake before use
Term
Antihistamines
Definition
-Alkylamines
-Ethanolamines
-Phenothiazines
-piperidines
-piperazines
Term
Alkylamines
Definition
Moderately sedating, strong anticholinergic effects, higher risk of paradoxical CNS stimulation compared with other classes.
-brompheniramine
-chlorpheniramine
-dexbrompheniramine
-dexchlorpheniramine
-pheniramine
-triprolidine
Term
Ethanolamines
Definition
Highly sedating, strong anticholinergic effects, large doses cause seizures and arrhythmias
-clemasine
-diphenhydramine
-doxylamine
Term
Ethylenediamines
Definition
Weak CNS effects, increase GI effects
-pyrilamine
-tripelennamine
-thonzylamine
Term
Phenothiazines
Definition
Highly sedating, strong anticholinergic effects, block alpha-adrenergic receptors, more likely to cause hypotension, akathisia and dystonic reactions may occur
-promethazine
Term
Piperidines
Definition
Non-sedating
-fexofenadine
-loratadine
-phenindamine
Term
Piperazines
Definition
Minimally to moderately sedating
-cetirizine
-chlorcyclizine
-hydroxyzine
-levocetirizine
-meclizine
Term
Decongestants
Definition
-common with allergic rhinitis
-can treat with systemic decongestants or short term ≤5 days of topical nasal decongestants
-effective for congestion, but litle effect on other symptoms
Term
Nasal Cromolyn (NasalCrom)
Definition
-prevents allergic rhinitis
--> use before exposure-stabilizes mast cells
--> initial effect 3-7 days, maximum effect 2-4 weeks
-less effective than intranasal corticosteroids
-simiar efficacy to antihistamines
-more effective than placebo
-ADRs: sneezing, brief nasal burning or stinging, nose bleeds, wheezing
-≤2 years of age
Term
When to seek medical attention regarding allergic rhinits
Definition
-symptoms worsen on OTC medication
-no improvement in 2-4 weeks of treatment
-secondary bacterial infection:
--> non-clear, thick nasal or respiratory secretions
--> temperature > 101.5F
--> SOB
--> Chest congestion
--> wheezing
--> ear pain
--> rash
Term
Allergic rhinitis conjunctivitis
Definition
-oral antihistamines
-intraocular antihistamines
-saline
Term
Nasal corticosteroids: Budesonide, fluticasone, triamcinalone (nasal) allergic effects in pregnancy
Definition
-facial clefts in some studies
Term
Piperazines and Piperadine allergic effects in pregnancy
Definition
-not expected to increase the risk of malformations
Term
Nasal corticosteroids: Budesonide, fluticasone, triamcinalone (nasal) allergic effects on lactation
Definition
-infant exposure expected to be minimal
-considered compatible with breastfeeding
Term
Fexofenadine effects on lactation
Definition
-lack of sedation and low milk levels--> no expected to cause any adverse effects in breastfed infants
-might have a negative effect on lactation
Term
Cetirizine effects on lactation
Definition
-Small occasional doses of cetirizine are probably acceptable in breastfeeding
-larger doses/prolonged use= may cause drowsiness and other effects in the infant or decrease the milk supply
Term
Loratadine effects on lactation
Definition
-lack of sedation and low milk levels--> no expected to cause any adverse effects in breastfed infants
-might have a negative effect on lactation
Term
Issues with drugs in pregnancy
Definition
-49% of pregnancies are unintended
-women listen to the negative effects of drugs that are not harmful (25% increase)
-Underying illness associated with maternal, fetal and neonatal morbidity and mortality
-PK and PD are altered in pregnancy
-Timing of exposure matters
Term
New pregnancy labels
Definition
-pregnancy including labor and delivery
-lactation including nursing mothers
-female and male reproductive potential
Term
Normal pregnancy duration
Definition
37-42 weeks, average is 40 weeks
Term
Embryonic/fetal development stages
Definition
1. Zygote
2. bilaminar embryo
3. embryonic period
4. fetal period
Term
Most organs have developed in the fetus after __weeks
Definition
8
Term
Changes during pregnancy
Definition
Increased: CYP3A, CYP2C9, CYP2D6, UGT, P-gp, OCT2, CrCl
Decreased: CYP1A2, possibly CYP2C19
Term
Good references for drug toxicity during pregnancy
Definition
-Drugs in pregnancy and lactation (Briggs)
-Reprotox
-Teris
-Product label if updated drug, if not, the label is not useful
Term
Drugs that should not be given during pregnancy
Definition
1. Thalidomide (25% major malformations)
2. Isotretinoin (50% major human teratogen)--wait one month before trying to get pregnant
3. Mycophenolate (Immunosuppressant for transplant patients) (27% malformations in patients): microtia (small head), cleft lip and palate, hypoplastic nails, shortened fingers, external auditory duct atresia, diaphragmatic hernias, heart malformations
Term
Malformation risk_______ when underlying conditions are uncontrolled
Definition
increase
Term
Macrosomia
Definition
Long term complications
-higher rate of impaired glucose tolerance at 2-5 years
-higher rate of type 2 diabetes
-higher rate of metabolic syndrome
-childhood obesity
Term
Should sertraline be used in pregnancy?
Definition
-Yes--does not adversely affect outcome. Depression should be treated!
-has risk of neonatal pulmonary hypertension in some studies
-has risk if reuptook late in pregnancy: of mild transient neonatal syndrome of CNS, motor, respioratory, and GI signs
Term
Benefits of breastfeeding
Definition
-maternal-neonatal bonding
-uterine contraction and decreased risk of bleeding
-increased IQ in offspring (possibly)
-complete nutrition for 1st 6 months, except possibly vitamin D
-Less odor from neonatal bowel movements
-decreased cost
Term
Breastfeeding prevents/reduces risk of
Definition
-middle ear infections
-respiratory tract infections
-colds and infections
-gut infections
-intestinal tissue damage
-sudden infant death syndrome
-allergic diseases
-celiac disease
-IBD
-Diabetes
-childhood leukemia
Term
3 methods of drug transfer into breast milk
Definition
1. Closed junction transcellular diffusion
2. Open junction paracellular diffusion
3. Milk fat paracellular diffusion
Term
Breast milk and maternal plasma pH
Definition
-breast milk: 7.0
-maternal plasma: 7.4
Term
Factors that influence movement of drugs to breast milk
Definition
-maternal plasma level the higher the plasma level, the higher the breast milk concentration
-Protein binding: only unbound drug crosses, lower protein concentration in milk
-lipid solubility: more likely to cross
-acid/base: weak bases transfer to acidic milk and then are trapped
-MW: higher MW (than 800Da--like insulin or heparin) are too large to cross the alveolar acini (glandular tissue where milk is produced)
Term
Factors in infant toxicity in breast feeding
Definition
-the dose in breast milk relative to the therapeutic amount
-the amount absorbed by a nursing infant
-the infant's ability to clear the drug
Term
Relative infant dose (RID) calculation
Definition
Infant dose (mg/kg/day)/maternal dose(mg/kg/day)
-RID is usually safe under 10%
Term
Colostrum
Definition
-24-48hours
-teaspoons
-low in fat
-high in carbs, protein and secretory IgA
Term
Foremilk
Definition
-beginning of feeding
-oz
-low in fat
-high in volume
Term
Hindmilk
Definition
-end of feeding
-higher in fat
Term
Different drugs are absorbed differently in different milks in the breastfeeding process: T or F?
Definition
True, sampling data is not easily correlated with this due to the collection of samples being at different stages of the feeding process.
Term
Best resource for medication safety during lactation
Definition
LactMed
Term
Is codeine safe during lactation?
Definition
NO!!! Even though RID is <1.4% (less than 10)
-codeine is a precursor of morphine--2005 baby died of morphine toxicity
Term
Is it okay for lactating mothers to give wait a few hours after taking their medication to nurse to avoid drug meeting the maximum concentration that could be passed on to the infant?
Definition
-No, peak concetrations of drug can be met 2 hours after taking the drug! The peak is unpredictable!
-Also note that outliers in RIDs may be above the 10% cut-off, but are still safer when considering that the infant plasma levels measured are usually lower
Term
Infant age affects the types of metabolizing enzymes present? T or F?
Definition
True, CYP450 for example is only present for about 24 hours and other enzymes develop thereafter with organ development= this changes the ability to metabolize drugs!
Term
Can sertraline be taken during lactation?
Definition
-Yes, little risk of withdrawal effects when some is lost in breastmilk
-since the baby has already been exposed, they have a lower risk of poor neonatal adaptation than if they were not exposed
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