routes of drug administration
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Routes of Drug Administration. Robert L. Copeland, Ph.D. Department of Pharmacology www.med.howard.edu/pharmacology 202.806.6311. Drug Absorption. Absorption is the process by which a drug enters the bloodstream without being chemically altered - PowerPoint PPT PresentationTRANSCRIPT
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Routes of Drug Administration
Robert L. Copeland, Ph.D.Department of Pharmacologywww.med.howard.edu/pharmacology 202.806.6311
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Drug Absorption Absorption is the process by
which a drug enters the bloodstream without being chemically altered
The movement of a drug from its site of application into the blood or lymphatic system
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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
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Ion Trapping: Kidney: Nearly all drugs filtered at the glomerulus: Most drugs in a lipid-soluble form will be absorbed by passive diffusion. 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)
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Routes of Drug Administration
The route of administration (ROA) that is chosen may have a profound effect upon the speed and efficiency with which the drug acts
ImportantImportantInfoInfo
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The possible routes of drug entry into the body may be divided into two classes:
EnteralParenteral
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Enteral Routes
Enteral - drug placed directly in the GI tract:sublingual - placed under the
tongueoral - swallowing (p.o., per os)rectum - Absorption through the
rectum
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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
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Sublingual/Buccal
Disadvantages inconvenient small doses unpleasant taste of some drugs
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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
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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
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Oral Disadvantages cont.
destruction of drugs by gastric acid and digestive juices
effect too slow for emergenciesunpleasant taste of some drugsunable to use in unconscious
patient
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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
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1. unconscious patients and children 2. if patient is nauseous or vomiting 3. easy to terminate exposure 4. absorption may be variable 5. good for drugs affecting the bowel such as laxatives6. irritating drugs contraindicated
Rectal
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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
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Intravascular
Absorption phase is bypassed (100% bioavailability)1.precise, accurate and almost immediate onset of
action, 2. large quantities can be given, fairly pain free
3. greater risk of adverse effects a. high concentration attained rapidly b. risk of embolism c. OOPS factor or !@#$%
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Intramuscular
1. very rapid absorption of drugs in aqueous solution 2.repository and slow release preparations 3.pain at injection sites for certain drugs
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Subcutaneous
1. slow and constant absorption 2. absorption is limited by blood flow, affected if circulatory problems exist 3. concurrent administration of
vasoconstrictor will slow absorption
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1.gaseous and volatile agents and aerosols 2.rapid onset of action due to rapid access to circulation a.large surface area b.thin membranes separates alveoli from circulation c.high blood flowParticles larger than 20 micron and the particles impact in the mouth and throat. Smaller than 0.5 micron and they aren't retained.
Inhalation
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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.
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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
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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)
Route for administration -Time until effect-
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Time-release preparations
Oral - controlled-release, timed-release, sustained-release designed to produce slow,uniform
absorption for 8 hours or longerbetter compliance, maintain effect
over night, eliminate extreme peaks and troughs
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NoNo single method of drug single method of drug administration is ideal for all administration is ideal for all drugs in all circumstancesdrugs in all circumstances
Very ImportantVery Important
Info!Info!