Routes & Formulations Flashcards
Formulations or Dosage Forms
Drugs are contained in dosing units
Route of Administration
A way of getting a drug into or onto the body.
- Enteral
- Parenteral
Enteral
Refers to anything involving the stomach from the mouth to the rectum
Parenteral
Routes other than enteral
Enteral Formulations
- oral (po)
- sublingual (sl)
- buccal
- rectal (pr)
Parenteral Formulations
- intravenous (IV)
- intramuscular (IM)
- ophthalmic
- intranasal
- inhalation
- dermal
- vaginal
Factors Affecting Selection of Route & Method of Administration
- Drug characteristics
- Ease of administration
- Site of action
- Onset of action
- Duration of action
- Quantity of drug administered
- Liver or kidney diseases
- Drug Characteristics
pH Scale
- measures the acidity of the alkalinity of a substance
- pH 7 is neutral (water)
- stomach is very acidic (pH 1-2)
- certain drugs are degraded or destroyed by stomach acids
- absorption of many drugs is affected by the presence of food in the stomach
- Drug Characteristics
pH Level
- stomach if very acidic (pH 1-2)
- duodenal pH is higher (closer is neutral)
- colonic pH is neutral to slightly alkaline
- Drug Characteristics
Drug Research Process
The influence of drug characteristics is examined and the formulations approved will have compensated for this
- Ease of Administration
- prescribers assess patient characteristics to determine route of administration
- difficulty in swallowing?
- consider liquid dose forms or non-oral routes of administration
- PO route may be inadvisable for patients w/ nausea and vomiting
- Site of Action
- route of administration may be influenced by desired site of action
- local effect
- systemic effect
- Site of Action
Local Effect
Site of drug activity and administration are one in the same
e.g. eyes, ears, nose, skin
- Site of Action
Systemic Effect
The drug is introduced into the circulatory system by any route of administration and carried by the blood to the site of action
- Onset of Action
Oral Medication
Since oral medications for systemic use need to go into solution to exert their effect, solutions or suspensions may work faster than oral tablets or capsules
- Onset of Action
Buccal or Sublingual (SL)
Medications placed under tongue or between cheek and gums work quickly because they bypass stomach and liver and go directly into bloodstream
- Onset of Action
IV
Drugs given IV directly are carried immediately throughout the body
- Onset of Action
Localized Therapeutic Effects
Those applied to the skin, inhaled into the lungs or instilled into eye
- Duration of Action
Length of time a drug gives the desired effect or is at the therapeutic level
- Duration of Action
Controlled or Extended Release
Drug effect lasts longer
e.g. 12 to 24 hrs
- Duration of Action
Transdermal Patches
Delivers small amounts of a drug steadily over many hours or even days
- Duration of Action
IV
Sustained duration effect can be achieved by means of intravenous infusion
- Duration of Action
IM and SQ
Injections into the muscle and skin last longer than injections directly into the bloodstream
- Quantity of Drug
- sometimes route of administration is chosen because of the amount of a drug
- IV infusion is an excellent method for systemic delivery of large quantities of material
- IV injections and infusions can deliver a higher dose of medication to the target site
- Metabolism by the Liver or Excretion by the Kidney
Liver Metabolism
Breaks down active drug to inactive metabolites for elimination and prevents drug accumulation
- Metabolism by the Liver or Excretion by the Kidney
First-pass Effect
- is the extent to which a drug is metabolized by the liver before reaching systemic circulation
- influences activity of some drugs
- such drugs have to be given in larger oral doses or by different route to bypass metabolism by the liver
- Metabolism by the Liver or Excretion by the Kidney
Effects of Age or Disease-related Change
- age or disease-related changes in liver or kidney function can cause:
- drug accumulation
- and potential toxicity
- drug dosage often needs adjustment in the elderly
- Metabolism by the Liver or Excretion by the Kidney
Multiple Potent Prescription
If patients are on multiple potent prescription drugs, there is a risk of a drug-drug interaction
- drug accumulation
- toxic blood levels increases
Oral Dosage Forms
Disintegration
The breaking apart of a tablet into smaller pieces
Oral Dosage Forms
Dissolution
When the smaller pieces of a disintegrated tablet dissolve in solution
Inactive Ingredients
- include binders, lubricants, fillers, diluents, and disintegrates
- added to help manufacture the formulation & to help the dosage form disintegrate & dissolve when administered
Most Frequent Route of Administration
- is PO
- oral refers to two method
- applying topically to the mouth for local effect
- swallowing for absorption through the GI tract into systemic circulation
Common Dose Form for Enteral
Solid Formation
- tablets
- capsule
- bulk powders
- rectal formulations
Tablet - Bulk Powders
Contain the active drug in a small powder paper or foil envelop. The patient empties the envelop into glass of water or juice and drinks the contents
Tablet - Chewable Tablets
Are flavored and are designed to be chewed
Tablet - Effervescent Tablets
Are granular salts that release gas and the active ingredient into solution when placed in water or juice
Capsules
- a solid dosage form consisting of a gelatin shell that encloses the drug
- usually swallowed whole
- tasteless and are easier to swallow than tablets
- contains powders, granules, liquids, or some combo w/ one or more active ingredients
- flavorings are not common for this dose form
Capsule - Soft or Soft-gel
Are capsules that contain liquid instead of powders inside the gelatin shell
Buccal Tablets and Gum
- placed in the buccal pouch
- between the cheek and the gum
- dissolved and absorbed by the buccal mucosa
Oral Dose Form
Delayed-release
- does not release the active drug immediately after administration
- avoid destruction in the stomach
- reduce GI upset
Oral Dose Form
Extended-release
Allows reduced frequency of dosing