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ROUTE OF DRUG ADMINISTRATION Julaeha, M.P.H., Apt
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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
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The possible routes of drug entry into the body may be divided into two classes:
Parenteral Enteral
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Routes of Administration
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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
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I. PARENTERAL A. Intravenous B. Intra-arterial C. Intramuscular
Injection sites for IM administration From: Fundamentals of Nursing, 4th edition, Lippincoitt, Williams & Wilkins
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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 (penyumbatan pembuluh darah)
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Intramuscular very rapid absorption of drugs in aqueous solution
Repository (tempat penyimpanan) and slow release preparations pain at injection sites for certain drugs Z-track method for IM injections
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Subcutaneous slow and constant absorption
Sites for SC injection slow and constant absorption absorption is limited by blood flow, affected if circulatory problems exist concurrent (bersamaan) administration of vasoconstrictor will slow absorption
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Aradigm Intraject® NFI device in protein delivery
Reproduced from:
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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
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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 destruction of drugs by gastric acid and digestive juices effect too slow for emergencies unpleasant taste of some drugs unable to use in unconscious (tidak sadar) patient
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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 Disadvantages inconvenient small doses unpleasant taste of some drugs
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Isosorbide concentrations after a 5 mg oral or sublingual dose.
Data from: Assinder et al. J Pharm Sci 66:775, 1977.
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Rectal unconscious patients and children
if patient is nauseous or vomiting easy to terminate exposure absorption may be variable good for drugs affecting the bowel (bag paling bawah) such as laxatives irritating drugs contraindicated
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avoid first-pass effect
RECTAL ROUTE Local action e.g. rectal route is used primarily for the treatment constipation Systemic action Advantage avoid first-pass effect
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VAGINAL ROUTE local action systemic action Marketed preparations include several feminine hygeine preparations, contraceptives, and labor inducing drugs. Advantage avoid first-pass effect Disadvantage The thickness of the vaginal epithelium and the blood circulation in this region changes with menstrual cycle and age, and the drug absorption also changes accordingly.
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Dosage forms suitable for vaginal route
tablet suppository ointment gel solution emulsion foam
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Pharmacologic Agents Administered
III. PULMONARY Pharmacologic Agents Administered via Inhalation For Systemic Effects pentamidine halothane ergotamine methoxyflurane enflurane isoflurane nitrous oxide For Local Effect beclomethasone terbutaline cromolyn metaproterenol albuterol pirbuterol
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Inhalation/Pulmonary
gaseous and volatile agents and aerosols rapid onset of action due to rapid access to circulation large surface area thin membranes separates alveoli from circulation high blood flow Particles larger than 20 micron and the particles impact in the mouth and throat. Smaller than 0.5 micron and they aren't retained.
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Forms of pulmonary delivery
Metered dose inhaler Dry powder inhalers Nebulizer
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Metered Dose Inhaler (MDI)
Metered-dose inhalers (MDI) provide medication with compressed gas deliver specific measured dose with each activation typical MDI
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Techniques for use of MDI devices:
Use of space or holding chamber Placement of inhaler in mouth (not for use with steroids) Two finger width from mouth Patient must coordinate inhalation and actuation of device
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Dry Powder Inhalers (DPI)
Breath activated Micronized drug particles blended with an excipient (e.g., glucose or lactose) Physical properties of drug and excipient critical (i.e., particle size, shape, surface morphology, etc)
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Diskus
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Nebulizer Device produces small droplets from a suspension or solution through an air jet or ultrasonic atomization (quieter, but more expensive)
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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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The skin is generally described in terms of three tissue layers:
stratum corneum epidermis dermis subcutaneous fatty tissue
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Dosage forms suitable for skin/transdermal route.
cream and ointment transdermal patch e.g. scopolamine trsansdermal patch
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Factors that influence percutaneous absorption
Site of application Condition of skin Hydration of skin Temperature Vehicle
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B. Ocular local action systemic action
The cornea of the eye has one of the highest nerve densities in the human body, as a result patients perceive pain and discomfort even at low thresholds of stimulation. From: Fundamentals of Nursing, 4th edition, Lippincoitt, Williams & Wilkins
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Types of Ophthalmic Preparations
Solutions Suspensions Ointments Inserts Intraocular solutions
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Factors that influence ocular drug retention
Technique of application
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Factors that influence ocular drug retention
Technique of application Drop size (volume) Formulation (tonicity, viscosity) pH of solution
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Route for administration
-Time until effect- intravenous seconds intraosseous seconds endotracheal 2-3 minutes inhalation 2-3 minutes sublingual 3-5 minutes intramuscular minutes subcutaneous minutes rectal 5-30 minutes ingestion minutes transdermal (topical) variable (minutes to hours)
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$65.55 Which route is best? $143.11 $143.11 $41.71
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Makaciiii
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