Routes of Administration Flashcards
Most desirable RoA is what?
At the drug’s site of action if this is possible
Decrease side effects, decrease dose, decrease cost, immediate action, maximum bioavailability
What do we need to consider for patient-specific RoA?
Age and physical condition
What do we need to consider for specific drugs’ routes of administration?
First pass effect, solubility, stability, absorption, dose (IV for large doses)
What do we need to consider with regards to diseases for routes of administration?
Systemic or local effects
Time of action
Sublingual dosage form, DoA, and onset
Tablets and drops
1-3 minute onset
30 minute DoA
Ointment dosage forms, DoA, and onset
Dosage forms = transdermal patch (40-60 minute onset, 18-24 hour DoA)
Dosage form = ointment (20-60 minute onset, 4-8 hour DoA)
IV infusion onset, and DoA
Parenteral solution
Immediate onset
DoA = several minutes
Buccal dosage forms, onset, and DoA
Extended release tablets
2-3 minute onset
DoA = 5 hours
Translingual dosage forms, onset, and DoA
Dissolving tablets (Onset = 2-4 min, DoA = 30-60 minutes) Extended release tablets (Onset = 20-45 min, DoA = 8-12 hours)
Advantages of oral route of administration
Systemic/local effect
Safe
Comfortable
Different release rates
Disadvantages of oral route of administration
First pass effect - lower bioavailability
Unpredictable absorption
If a drug is given in soluble form or it dissolves rapidly, what is the rate limiting step for its absorption?
Membrane transport
If rate of dissolution is slow, what might happen to the drug?
The drug may not be absorbed to a sufficient extent
What are the two factors that affect drug dissolution and release in the oral route of administration
Formulation and intrinsic dissolution
Rank these dosage forms in terms of dissolution: Tablets, solutions, suspensions, capsules
Solutions > Suspensions > Capsules > Tablets
What does intrinsic dissolution refer to?
The ability of the drug (not the formulation) to dissolve
What factors affect intrinsic dissolution? How do they affect it?
Increase in temperature (can increase or decrease saturated solubility, increases diffusion coefficient)
Viscosity of medium (decreases diffusion coefficient - dissolution will decrease if viscosity increases)
Agitation (decreases thickness of diffusion layer therefore increasing dissolution rate)
Change in pH (Changes saturated solubility)
Reduction of size (surface area for dissolution)
What factors affect solubility?
Polymorphism (forming complexes with ions - can increase duration of action)
Hydrated vs. anhydrous form
Salt form (usually more solubility, but some have less solubility - like penicillins)
What are the four major mechanisms of drug entry into cells?
- Diffusion (high concentration to low concentration - ONLY unionized drugs can pass membrane via diffusion because positive drugs will be trapped by membrane and negative charged drugs will be repelled)
- Facilitated diffusion (high concentration to low concentration using carrier or channel proteins)
- Active transport (uses ATP - low concentration to high concentration for water soluble or large molecules)
- Exocytosis or endocytosis (slow and inefficient, minor route for drug absorption)
What are ABC efflux proteins?
“Gatekeepers” - limit amount of drug entering cell
Works against drug absorption
In terms of membrane permeability, what are other factors that affect drug absorption from the oral route?
Age (increases or decreases permeability/absorption)
Disease of GI tract
Lipophilicity of drug
Surface area (particle size)