Lecture 2: Basic Principles of Pharmacology II Flashcards
What forms of drugs can easily diffuse?
Nonionized forms
What forms of drugs do not diffuse?
Ionized forms
What are the 2 types of routes of administration?
- Enteral (Oral, Rectal, Sublingual)
2. Parenteral (Intravenous, Intraarterial, Intramuscular, Subcutaneous, Intrathecal, Topical, Inhalation)
What are some of the advantages of oral administration?
Easy, safe, prolonged absorption causing prolonged effect
What are some of the disadvantages of oral administration?
- Absorption may be too slow
- Absorption variable and unpredictable
- Drugs can be completely metabolized on first pass through liver
- Not available for comatose, vomiting patients.
What are some advantages of rectal administration?
- Useful for infants, comatose, vomiting pts
- Useful for foul-smelling, distasteful drugs
- Useful for drugs destroyed in upper gastrointestinal tract
- Avoids immediate metabolism liver
What are some of the disadvantages of rectal administration?
- Nuisance - poor compliance
- Absorption may be erratic, incomplete
- Rectal irritation
What are some of the advantages of sublingual administration?
- By-basses liver when first absorbed
2. Rapid absorption
What are some of the disadvantages of sublingual administration?
- Must be soluble in saliva, have appropriate pKa rapid absorption
- Tablets must be small
Advantages of intravenous administration?
- Rapid effect
- Can watch response and titrate dose
- For drugs given in large volumes of fluid and continuous monitoring
What are some of the disadvantages of intravenous administration?
- Cost
- Danger of infection
- Possible anaphylactic rxn
- Danger of embolus formation due to air, drug precipitation, RBC agglutination
- Danger of adverse cardiovascular effects if administration too rapid
Advantages of intraarterial route?
- Administration of radioopaque material for visualization of circulatory tree
- High conc. of drug going to local when desirable
Disadvantages of the intraarterial administration?
As for iv administration
What are some of the advantages of intramuscular?
- When oral route is not available
- Absorption less variable than with oral route
- Absorption more rapid with s.c. route
- Possibility of slowing absorption to prolong effect
Disadvantages of intramuscular route?
- Possible local necrosis
- Accidental i.v. injection possible
- Should not be used after anticoagulant administration
Advantages of subcutaneous route?
- Absorption usually slower than after i.m., and effect more prolonged
Disadvantages of subcutaneous route?
As for i.m. administration
Advantages of intrathecal?
When local effect on CNS required other route unsatisfactory
Disadvantages of intrathecal?
- Skill
2. Danger of spinal cord injury
Advantages of topical?
- for local action on or under skin
2. non-invasive
Disadvantages of topical route?
- Difficulty of absorption through skin
2. Danger of excessive absorption through membranes and systemic toxicity
Advantages of inhalation route?
- Rapid absorption for systemic action
- High conc. attainable for local effect
- Self administration possible
Disadvantages of inhalation route?
- Possible excessive absorption and systemic toxicity
- Poor regulation of dosage
- Irritation of pulmonary
Define bioavailability
Fraction of dose available for biologic action
What are the characteristics of bioavailability?
- Pertains to oral drug administration where variable absorption or “first pass” effects will decrease the amount of drug which reaches the circulation
- Measured by comparing the AUC (area under the curve) for the oral dose form vs the intravenous dose form.
(FA) True or false
Ionized species are trapped in urine and cleared quickly.
True
(FA) True of false
Neutral forms can be reabsorbed
True
(FA) What are some of the examples of weak acids drugs?
Phenobarbital, methotrexate, aspirin
(FA) What are the characteristics of weak acid drugs?
- They are trapped in basic environment
2. Treat overdose with bicarbonate
(FA) What are some of the examples of weak base drugs?
Amphetamines
What are the characteristics of weak base drugs?
- They are trapped in acidic environments.
2. Treat overdose with ammonium chloride.
Protein bound drug can’t cross
the capillary membrane
Weak electrolyte drugs can be either
nonionized form or ionized form / weak acids or base
Nonionized form
diffuse
ionized form
do not diffuse
pKa will help
to figure out ionized/nonionized form
Drug administration could be either
enteral or parenteral
What are some of the considerations for routes of administraiton?
- Planned use of medication
- Clinical setting - acute vs. chronic
- Rapidly of onset of desired action
- Specific target organ that the drug is intended to reach
Parenteral means
you bypass the GI tract
Enteral means
you use part of the GI tract
What is the most advantage of oral administration?
Prolonged and maintain steady conc.
Disadvantages of oral route?
The drugs have to pass the liver and will destroyed.
Liver metabolism of the drug is called
First pass metabolism (effect)
Advantages of rectal?
useful for comatose, vomiting pt. via suppository
Sublingual route advantages?
- By-passes liver when first absorbed
- Rapid absorption
- Tablets or sprays
What kind of drug shows a strong first pass effect?
Opioid agonists are bio transformed in the liver by CYP450 enzymes
Advantages of IV route?
- Rapid effect
2. Can titrate dose
Disadvantages of IV route?
- Danger of adverse cardiovascular effects if administration is too rapid
- Formation of embolus
Advantages of intraarterial route?
administration of radio material or a specific location in the brain
Advantages of IM (Deep muscle) route?
when oral is not available, to slow absorption to prolong effect
Advantages of SC?
Look at the note
Advantages of intrathecal
when local effect on CNS required and other route unsatisfactory, usually for analgesia
Advantages of inhalation?
- high conc attainable for local effect (lung–> albutalol)
- Rapid absorption for systemic action
- Very close to i.v. absorption for volatile gases such as anesthetics or toxic gases
Inhalation absorption will be
just below IV on a graph (plasma levels of drug vs. time)
Advantages of subcutaneous
absorption usually slower than i.m.