Pediatric & Geriatric Pharmaceutics Flashcards
Define Paediatric Pharmaceutics.
Branch of pharmaceutical science specific to the use if medication in children, including dosage forms, pharmacokinetics/pharmacodynamics and special medicinal needs appropriate to young patients/consumers
In 1999, the FDA established regulations regarding labelling o new products for the safety of children. What else did the new regulations allow the FDA to do?
Require pediatric testing of-already marketed drugs when the drug is frequently prescribed to children.
List the five subgroups of pediatric population based on age.
Intrauterine- conception to birth Neonate- birth to 1 month Infant- 1 month to 2 years Child- 2 years to onset of puberty Adolescent- onset of puberty to adult
How are the most accurate doses decided for paediatrics?
Utilizing age and weigh
*surface area has no practical advantage
Does gastric acid output increase or decrease with age?
Lowest gastric acid output is observed in neonate of 10-30 days. Values approach adult levels by three months.
What other physiological features affect absorption in Neonates?
Gastric emptying time and intestinal transit time are erratic in Neonates. Pancreatic enzyme activity is low (lipid soluble drugs poorly absorbed).
When does the colonization and metabolic activity of GI flora approach adult values and what drug has an increased bioavailability due to this?
2-4 yrs
Digoxin
What reactions in metabolism are delayed in Neonates but are adult level by 4-6 months?
Phase 1 reactions
Oxidation, n-demethylation
When do conjugation pathways approach adult values?
3-4 yrs, can see prolonged half lives
What does renal excretion of drug depend on?
Glomerular filtration, tubular secretion and tubular absorption
When does tubular secretion approach adult values?
Between 2 -6 months, greatest variability of drug disposition
How do adverse reactions differ in the pediatric population?
In type and incidence, due to immature metabolic pathways
Ex) theophylline, antibiotics, antihistamines
What excipients/additives can be an issue in pediatric patients?
Dyes and sweeteners; hypersensitivity
Give example of dyes that are known for hypersensitivity reactions.
FD&C Yellow #5 and #6
Tartrazine-induced bronchoconstriction (ASA-cross sensitivity)
What is the most popular sweetener?
Sucrose
Chewable may contain up to 20-60%
Liquids may contain up to 85%
This preparation can represent a substantial carbohydrate load to children with diabetes.
Oral liquid
Why is lactose not recommended as a sweetener pediatric populations?
High incidence of lactose intolerance.
This ingredient is second only to water in its use in liquid preparations, acting a preservative and flavoring agent.
Ethanol
May also enhance the oral absorption of some active ingredients
What is the largest level of ethanol in the blood suggested for children in single dose?
25mg/dL because they have a limited ability to metabolize and detoxify ethanol
What is the preferred route of administration for children?
Oral administration
Younger than what age have difficulty or are unable to swallow solid oral dosage forms?
5 years old
What are the downsides to liquid dosages?
Unstable and have short half lives.
Difficulty in accurate measurement and administration
What is an alternative formulation that is widely accepted by children under three and their parents?
Chewable tablets and sprinkle capsules
Consider the benefits and the risks of rectal administration in paediatrics.
Wide variability in the rate and extent of absorption in children
Inflexibility of fixed dose.
Not promoted for paediatrics
Consider the benefits and the risks of transdermal administration in paediatrics.
Stratum corneum is fully developed at birth ad similar permeability to adults.
Preterm Neonates have underdeveloped epidermal barrier and are at risk for excessive absorption.
Consider the benefits and the risks of parenteral administration in paediatrics.
IM injection absorption is erratic in Neonates (small muscle mass, inadequate perfussion)
Amount of volume directly related with discomfort (too small=isotonic, too large= multiple injection)
Consider the benefits and the risks of pulmonary administration in paediatrics.
Effective in pediatrics for local but systemic needs to be studied more.
What are important factors in the elopement of dosage forms for pediatrics?
Smell, taste, texture, and aftertaste
Cherry, orange, strawberry and bubblegum are most common
What is the critical void in pediatric drug therapies that remains?
Effective drug delivery systems
Define Geriatric Pharmaceutics.
Branch of pharmaceutical science specific to the use of medications in the elderly, including dosage forms, pharmacokinetics/pharmacodynamics and special medicinal needs appropriate to aging patients/consumers
Old age is defined as “advanced years of life when strength and vigor decline”. What are the official are classifications?
Young-old group: 65-74 yrs
Middle-old group: 75-84 yrs
Old-old group: over 85 yrs
What is the issue with enteric-coated formulations in elderly patients?
There is a decrease in gastric secretion, raising the pH, resulting in premature dissolution.
Elevated pH can also lead to incomplete absorption of weakly acidic compounds
What attribute to increase half-life of drugs through the liver in elderly patients?
Decreased hepatic blood flo, liver size and Phase 1 metabolism.
Increased incidence of liver dysfunction
What else will increase the half life due to slowed elimination?
Renal function deterioration
What are three physical limitations unique to the geriatric population that can interfere with effective drug delivery?
Dexterity (arthritis, tremors, natural frailty and weakness)
Vision (impaired, may hinder ability to self-administer medications)
Swallowing & Chewing (dry-mouth, loss of teeth, esophageal lesions, decreased bulk and tone of oral musculature)
What is the preferred formulation for elderly?
Solid dosage forms, particularly tablets
Consider the benefits and the risks of oral dosage forms for administration in geriatrics.
Chewable: not recommended, decrease chewing ability
Capsules: not recommended, mucosal adherence
SL and Buccal: reduced bioavailability due to dry mouth
Liqiuds: beneficial if difficulty swallowing solids, but accurate measurement needed.
Consider the benefits and the risks of transdermal dosage forms in geriatrics.
Elderly have decreased transdermal absorption because skin is different.
Consider the benefits and the risks of parenteral dosage forms in geriatrics.
Effective, but not well received due to invasiveness and administration
What are the six alternative delivery systems for geriatrics?
Granules: not effected by changes in gastric emptying rate
Coated tablets: less likely to adhere to esophageal mucosa, “caplets”
Effervescent tablets
Soluble tablets: placed in mouth and fast dissolving or placed in water
Gel preparations
Concentrated oral solutions: volume less than 5mL, can b mixed with food or drink. (Taste and poor solubility issues)
Why is patient compliance a major concern in the elderly?
Multiple medications, various physical impairments
How can we increase geriatrics adherence?
Taste preference
Package and label design (unable to open or cannot read, keep in mind elderly dexterity and visual decline)
What is included in a elderly friendly packaging?
Unit dose packages, avoiding tamper-proof containers
Use matte surfaces to minimize glare
Print instructions in light colours on dark backgrounds
Use distinct spacing between letters and increase thickness
What are one compliance aids that can be used in the elderly?
Calendar packs (when, what and why) Drug-reminder cards