You are on page 1of 40

Routes of Drug Administration

4/10/12

Drug Absorption
 Absorption

is the process by which a drug enters the bloodstream without being chemically altered or  The movement of a drug from its site of application into the blood or lymphatic system

Drug Absorption

Factors which influence the rate of absorption
 

    

types of transport the physicochemical properties of the drug protein binding routes of administration dosage forms circulation at the site of absorption concentration of the drug

Drug Absorption

The rate at which a drug reaches it site of action depends on:  Absorption - involves the passage of the drug from its site of administration into the blood  Distribution - involves the delivery of the drug to the tissues

Drug Absorption  Mechanisms   of solute transport across membranes passive diffusion filtration and bulk flow endocytosis ion-pairing active transport Drug Absorption animation     .

.

Ion Trapping cont: Body fluids where a pH difference from blood pH will favor trapping or reabsorption: stomach contents small intestine breast milk aqueous humor (eye) vaginal secretions prostatic secretions .

To increase excretion: change the urinary pH to favor the charged form of the drug: • Weak acids: excreted faster in alkaline pH (anion form favored) • Weak bases: excreted faster in acidic pH (cation form favored) .Ion Trapping: Kidney: Nearly all drugs filtered at the glomerulus: Most drugs in a lipid-soluble form will be absorbed by passive diffusion.

Lipid-Water Partition Coefficient  The ratio of the concentration of the drug in two immiscible phases: a nonpolar liquid or organic solvent (representing the membrane).4 (representing the plasma) . and an aqueous buffer. pH 7.

c. .Lipid-Water Partition Coefficient  The higher the lipid/water p.c. polarity of a drug.c. the greater the rate of transfer across the membrane   polarity of a drug. by increasing ionization will the lipid/ water p. suppression of ionization will the lipid/ water p.

Routes of Drug Administration Important Info The route of administration (ROA) that is chosen may have a profound effect upon the speed and efficiency with which the drug acts .

 The possible routes of drug entry into the body may be divided into two classes: 1)SYSTEMIC-  A)Enteral  B)Parenteral –  topical -deeper tissues arterial 2)LOCAL .

.drug placed directly in the GI tract:  sublingual .Absorption through the rectum .swallowing (p.o. per os)  rectum .Enteral Routes  Enteral .placed under the tongue  oral .

Sublingual/Buccal Some drugs are taken as smaller tablets which are held in the mouth or under the tongue.  Advantages    rapid absorption drug stability avoid first-pass effect .

Sublingual/Buccal  Disadvantages    inconvenient small doses unpleasant taste of some drugs .

Oral  Advantages    Convenient . pain free. easy to take Absorption .compared to most other parenteral routes .can be self.takes place along the whole length of the GI tract Cheap .administered.

Oral  Disadvantages    Sometimes inefficient .only part of the drug may be absorbed First-pass effect .drugs absorbed orally are initially transported to the liver via the portal vein irritation to gastric mucosa nausea and vomiting .

Oral  Disadvantages cont.     destruction of drugs by gastric acid and digestive juices effect too slow for emergencies unpleasant taste of some drugs unable to use in unconscious patient .

First-pass Effect  The first-pass effect is the term used for the hepatic metabolism of a pharmacological agent when it is absorbed from the gut and delivered to the liver via the portal circulation. The greater the first-pass effect. the less the agent will reach the systemic circulation when the agent is administered orally .

where Q is hepatic blood flow (usually about 90 L per hour. Magnitude of first pass hepatic effect: Extraction ratio (ER) ER = CL liver / Q . Systemic drug bioavailability (F) may be determined from the extent of absorption (f) and the extraction ratio (ER): F = f x (1 -ER) .First-pass Effect cont.

First-pass Effect .

absorption may be variable 5.Rectal 1. good for drugs affecting the bowel such as laxatives 6. if patient is nauseous or vomiting 3. easy to terminate exposure 4. irritating drugs contraindicated . unconscious patients and children 2.

NasalDigestive juices &liver are bypassed Examples-GnRH agonists.desmopressin .

drug injected into skeletal muscle Subcutaneous .placing a drug directly into the blood stream Intramuscular (IM) . IA).Absorption through the lungs .Parenteral Routes     Intravascular (IV.Absorption of drugs from the subcutaneous tissues Inhalation .

.

.

.Time until effect -intravenous 30-60 seconds -intraosseous 30-60 seconds .sublingual 3-5 minutes ..-intramuscular 10-20 minutes .inhalation 2-3 minutes .endotracheal 2-3 minutes .

30-90 minutes transdermal (topical) variable (minutes to hours)  .Time until effect-subcutaneous 15-30 minutes  .rectal 5-30 minutes ingestion  .

large quantities can be given.Intravascular Absorption phase is bypassed (100% bioavailability) 1. fairly pain free 3. accurate and almost immediate onset of action. risk of embolism c. greater risk of adverse effects a. OOPS factor or !@#$% . 2. high concentration attained rapidly b.precise.

pain at injection sites for certain drugs . very rapid absorption of drugs in aqueous solution 2.Intramuscular 1.repository and slow release preparations 3.

concurrent administration of vasoconstrictor will slow absorption .Subcutaneous 1. absorption is limited by blood flow. slow and constant absorption 2. affected if circulatory problems exist 3.

large surface area b.rapid onset of action due to rapid access to circulation a.5 micron and they aren't retained. Smaller than 0.gaseous and volatile agents and aerosols 2.high blood flow Particles larger than 20 micron and the particles impact in the mouth and throat.Inhalation 1.thin membranes separates alveoli from circulation c. .

     Respiratory system. freebase and crack cocaine. crystal meth. local damage to septum. Intranasal (snorting) Snuff. cocaine may be partly oral via postnasal dripping. Longer action than volatile gases. then diffuse. Some of the volatile gases also appear to cross nasal membranes. CO. petroleum distillates. Smoke (Solids in air suspension. Except for IN.Particles or vapors dissolve in lung fluids. Tissue damage from particles. ether) [precise control]. Lung-based transfer may get drug to brain in as little as five seconds. .Inhalation cont. opium. risk hypoxia. THC. vapors) absorbed across lung alveoli: Nicotine. Volatile gases: Some anaesthetics (nitrous oxide. tars. Diffusion and exhalation (alcohol). Fairly fast to brain.

) •Skin a. Dermal . no first pass metabolism iii. stable blood levels ii.absorption of drug through skin (systemic action) i. callous removal. nasal. etc. sunscreen. Transdermal . drug must be potent or patch becomes to large .rubbing in of oil or ointment (local action) b.Topical •Mucosal membranes (eye drops. antiseptic.

sustained-release  designed to produce slow.controlled-release. eliminate extreme peaks and troughs . timedrelease. maintain effect over night.Time-release preparations  Oral .uniform absorption for 8 hours or longer  better compliance.

parental administration (except IV).Time-release preparations  Depot or reservoir preparations . . may be prolonged by using insoluble salts or suspensions in non-aqueous vehicles.

at particular sites .Important Info The ROA is determined by - •the physical characteristics of the drug. •the speed which the drug is absorbed and/ or released. as well as • the need to metabolism and bypass hepatic •achieve high conc.

No single method of drug administration is ideal for all drugs in all circumstances .

.

Write down the 3 advantages and 3 disadvantages of any two routes. . 2) Classify routes of administration of drugs.Briefly discuss factors affecting drug absorption following oral route.1)Enumerate the various routes of drug administration.List advantages and disadvantages of Intrvenous route.