Administration drugs

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Routes of Drug Administration - Robert L. Copeland, Ph.D. Department of Pharmacology

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Administration drugs

  1. 1. Routes of Drug Routes of Drug Administration AdministrationRobert L. Copeland, Ph.D.Department of Pharmacologywww.med.howard.edu/pharmacology202.806.6311
  2. 2. 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
  3. 3. 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
  4. 4. 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
  5. 5. Drug Absorption Mechanisms of solute transport across membranes  passive diffusion  filtration and bulk flow  endocytosis  ion-pairing  active transport  Drug Absorption animation
  6. 6. Ion Trapping cont:Body fluids where a pH difference fromblood pH will favor trapping orreabsorption: stomach contents small intestine breast milk aqueous humor (eye) vaginal secretions prostatic secretions
  7. 7. Ion Trapping:Kidney: Nearly all drugs filtered at the glomerulus: Most drugs in a lipid-soluble form will be absorbedby passive diffusion.To increase excretion: change the urinary pH to favorthe charged form of the drug:• Weak acids: excreted faster in alkaline pH (anionform favored)• Weak bases: excreted faster in acidic pH (cationform favored)
  8. 8. 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); and an aqueous buffer, pH 7.4 (representing the plasma)
  9. 9. Lipid-Water Partition Coefficient  The higher the lipid/water p.c. the greater the rate of transfer across the membrane  polarity of a drug, by increasing ionization will the lipid/ water p.c.  polarity of a drug, suppression of ionization will the lipid/ water p.c.
  10. 10. Routes of Drug Administration Important InfoThe route of administration (ROA) that is chosen may have a profound effect upon the speed and efficiency with which the drug acts
  11. 11.  The possible routes of drug entry into the body may be divided into two classes: Enteral Parenteral
  12. 12. Enteral Routes Enteral - drug placed directly in the GI tract:  sublingual - placed under the tongue  oral - swallowing (p.o., per os)  rectum - Absorption through the rectum
  13. 13. Sublingual/BuccalSome 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
  14. 14. Sublingual/Buccal Disadvantages  inconvenient  small doses  unpleasant taste of some drugs
  15. 15. Oral Advantages  Convenient - can be self- administered, pain free, easy to take  Absorption - takes place along the whole length of the GI tract  Cheap - compared to most other parenteral routes
  16. 16. 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
  17. 17. 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
  18. 18. 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
  19. 19. First-pass Effect cont. Magnitude of first pass hepatic effect: Extraction ratio (ER)ER = CL liver / Q ; where Q is hepaticblood flow (usually about 90 L per hour.Systemic drug bioavailability (F) may bedetermined from the extent of absorption(f) and the extraction ratio (ER): F = f x (1 -ER)
  20. 20. First-pass Effect
  21. 21. Rectal1. unconscious patients and children2. if patient is nauseous or vomiting3. easy to terminate exposure4. absorption may be variable5. good for drugs affecting the bowel such as laxatives6. irritating drugs contraindicated
  22. 22. Parenteral Routes Intravascular (IV, IA)- placing a drug directly into the blood stream Intramuscular (IM) - drug injected into skeletal muscle Subcutaneous - Absorption of drugs from the subcutaneous tissues Inhalation - Absorption through the lungs
  23. 23. IntravascularAbsorption phase is bypassed(100% bioavailability)1.precise, accurate and almost immediate onset of action,2. large quantities can be given, fairly pain free3. greater risk of adverse effects a. high concentration attained rapidly b. risk of embolism c. OOPS factor or !@#$%
  24. 24. Intramuscular1. very rapid absorption of drugs in aqueoussolution2.repository and slow release preparations3.pain at injection sites for certain drugs
  25. 25. Subcutaneous1. slow and constant absorption2. absorption is limited by blood flow, affected if circulatory problems exist3. concurrent administration of vasoconstrictor will slow absorption
  26. 26. Inhalation1.gaseous and volatile agents and aerosols2.rapid onset of action due to rapid access tocirculation a.large surface area b.thin membranes separates alveoli from circulation c.high blood flowParticles larger than 20 micron and the particles impactin the mouth and throat. Smaller than 0.5 micron andthey arent retained.
  27. 27. Inhalation cont. Respiratory system. Except for IN, risk hypoxia. Intranasal (snorting) Snuff, cocaine may be partly oral via post- nasal dripping. Fairly fast to brain, local damage to septum. Some of the volatile gases also appear to cross nasal membranes. Smoke (Solids in air suspension, vapors) absorbed across lung alveoli: Nicotine, opium, THC, freebase and crack cocaine, crystal meth.Particles or vapors dissolve in lung fluids, then diffuse. Longer action than volatile gases. Tissue damage from particles, tars, CO. Volatile gases: Some anaesthetics (nitrous oxide, ether) [precise control], petroleum distillates. Diffusion and exhalation (alcohol). Lung-based transfer may get drug to brain in as little as five seconds.
  28. 28. Topical•Mucosal membranes (eye drops, antiseptic,sunscreen, callous removal, nasal, etc.)•Skin a. Dermal - rubbing in of oil or ointment (local action) b. Transdermal - absorption of drug through skin (systemic action) i. stable blood levels ii. no first pass metabolism iii. drug must be potent or patch becomes to large
  29. 29. Route for administration -Time until effect- intravenous 30-60 seconds intraosseous 30-60 seconds endotracheal 2-3 minutes inhalation 2-3 minutes sublingual 3-5 minutes intramuscular 10-20 minutes subcutaneous 15-30 minutes rectal 5-30 minutes ingestion 30-90 minutes transdermal (topical) variable (minutes to hours)
  30. 30. Time-release preparations Oral - controlled-release, timed- release, sustained-release  designed to produce slow,uniform absorption for 8 hours or longer  better compliance, maintain effect over night, eliminate extreme peaks and troughs
  31. 31. Time-release preparations Depot or reservoir preparations - parental administration (except IV), may be prolonged by using insoluble salts or suspensions in non-aqueous vehicles.
  32. 32. Important InfoThe ROA is determined by thephysical characteristics of thedrug, the speed which the drug isabsorbed and/ or released, as wellas the need to bypass hepaticmetabolism and achieve highconc. at particular sites
  33. 33. rtant Impo Very fo! InNo single method of drugadministration is ideal for alldrugs in all circumstances
  34. 34. THAT’S IT!!

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