Routes of Administration of Drugs.

Learning Objectives At the end of the lecture, the student should be able to : Describe the routes of administration of drugs. Give the advantages of the each of the route of administration of drug. Discuss the disadvantages of the drugs given by various routes. ROUTES OF DRUG ADMINISTRATION A drug can be given systemically & Locally. Systemic routes are divided into: ENTERAL: Oral, Sublingual, Rectal. PARENTERAL: Intravenous, Intramuscular, Subcutaneous. Intra-arterial, Intra-articular, Intra-dermal. INHALATIONAL. TOPICAL & LOCAL APPLICATION ORAL: Both liquid and solid dosage forms of a drug are swallowed; most commonly employed route of drug administration.

 Advantages Safe. Convenient. Economical. Drug absorption is good due to extensive surface area. Disadvantages

some drugs have slow absortion. Onset of drug action is slow. Irritable and unpalatable drugs can not be given. Not utilized in unconscious and uncooperative patients. Cannot utilize in severe vomiting. Some drugs are destroyed in stomach like insulin etc. Drugs after absorption are metabolized in liver before reaching the systemic circulation, this is called FIRST PASS EFFECT. Drug absorption affected by intake of food. Some drugs produce irritation to gastric mucosa. First-pass Effect

 SUBLINGUAL:Solid or liquid dosage form of drug is kept below the tongue for short period of time to be absorbed through oral mucosa.

Advantages economical ; specific apparatus or sterilization is needed. Quick termination of undesirable drug effects by spitting remaining drug. First pass effect is avoided. Drug absorption and effects are quick. Disadvantages Bitter tasting and unpalatable drug. Irritation of oral mucosa. can not give to unconscious patient. Large quantities can not be given. can not be given in severe vomiting.

 some drugs are absorbed through oral mucosa,like nitroglycerine. RECTAL: Solid and liquid forms of drugs can be given through rectum. solid drug given rectally is known as SUPPOSITORY. Liquid drug given rectally is called ENEMA.. Drugs are used to produce local or systemic effects. Advantages used in children. Little first pass effect. Can be given in vomiting. Can be given in unconscious patient. Higher therapeutic concentrations of drug are achieved rapidly in rectum. for rapid evacuation of bowel, usually during gut sterilization before any surgical or radiological procedure. Disadvantages inconvenient. Drug absorption is slow and erratic. Irritation or inflammation of rectal mucosa can occur.

PARENTERAL ROUTES Advantages Rapid onset of action. can be given to unconscious patients. Accuracy of dosage is ensured. Useful in emergency situations. First pass effect is avoided. Drugs producing gastric irritation can be given. Drugs that are not absorbed from G.I.T can be given. Drugs destroyed by gastric acid can be given. can be given in presence of vomiting and diarrhea. Disadvantages Less safe. side effects produced, are difficult to control. Technical person needed self-administration is difficult . Expensive. Inconvenient and painful. Chances of nerve and blood vessel damage. Danger of infection, if proper sterilization techniques are not used.

INTRAVENOUS

Advantages No absorption required; bioavailability is 100%. Desired blood concentration of drug is achieved quickly and can be maintained. Large volume of drug can be given. Rapid onset of action. Drugs can be given in presence of vomiting and diarrhea.

 INTRAVENOUS Advantages: Useful for unconscious patients. Useful in emergency situations. First pass effect is avoided. Drugs producing gastric irritation can be given. Drugs that are not absorbed from G.I.T can be given. Drugs destroyed by gastric acid can be given. INTRAVENOUS:

Disadvantages: Extravasation of drugs produces irritation and cellulitis. Chances of thrombophlebitis. Repeated I/V administration requires patent veins, sometimes that may not be possible. Less safe, once the side effects produced, they are difficult to control. INTRAVENOUS: Disadvantages: Technical person is needed, self-administration is difficult. Expensive. Inconvenient and painful. Danger of infection, if proper sterilization techniques are not used.

 INTRAMUSCULAR:

Drugs injected in deltoid muscle or gluteal region. Intramuscular injections are given at: deltoid, gluteus maximus and vastus lateralis.

Deep I/M injections are less painful than I/M injections on arm due to high fat content.

 INTRAMUSCULAR:

Absorption of drug from gluteal region is slow especially in females due to high fat deposition. Deep intramuscular injections are given at upper outer quadrant of buttock to prevent the injury to major nerves. Intramuscular injections are given at an angle of 90 degrees. Advantages Rate of absorption is uniform. Rapid onset of action. Irritant substances can be given. Drugs can be given to unconscious patients. Accuracy of dosage is ensured. Useful in emergency situations. First pass effect is avoided. Drugs producing gastric irritation can be given. Drugs that are not absorbed from G.I.T can be given. Drugs destroyed by gastric acid can be given. Disadvantages

 Small quantities up to 10 ml of the drug can be given at a time. Local pain and abscess formation. Technical person is needed, self-administration is difficult. Expensive. Danger of infection, if proper sterilization techniques are not used. Chances of nerve damage. SUBCUTANEOUS: Drugs are injected below the skin Advantages: Actions of the drugs are sustained and uniform. Drugs can be given in presence of vomiting and diarrhea. Drugs can be given to unconscious patients. First pass effect is avoided. Drugs that are not absorbed from G.I.T can be given. Disadvantages

Only non-irritant drugs can be given otherwise severe irritation, pain and necrosis of subcutaneous tissues can occur. Absorption of the drugs is slow than I/M injection. Expensive. Danger of infection, if proper sterilization techniques are not used. Large volumes of drug can not be given.

 INHALATION: Gases, volatile liquids and solids (in the form of finely divided powders) are inhaled for systemic and local effects. Inhalation of solids is called insufflation. Advantages Rapid absorption of the drug due to large surface area. First pass effect is avoided. Rapid local effects. Disadvantages Only few drugs can be administered. may produce irritation of pulmonary mucosa. Inconvenient procedure.

 Chances of cardiotoxicity. Systemic side effects may be produced due to rapid absorption of drug. Poor ability to regulate dose.

TOPICAL OR LOCAL APPLICATION Drugs may be applied to skin and mucous membrane of eye, ear, nose, throat, mouth, urinary bladder, vagina and rectum for local effects, this is called topical or local application. Drugs are given in the form of ointments, creams, lotions, and powders.

TOPICAL OR LOCAL APPLICATION Some drugs like nitroglycerin and scopolamine are absorbed through intact skin and are used to produce systemic effects, in the form of transdermal patches. Absorption of the drug through skin can be increased by suspending the drug in oily vehicle and rubbing the resultant preparation on skin, this method is called innunction.

INTRAVESICULAR

Agents used: Mitomycin, Doxorubicin, Instilled into bladder via catheter Side effects: excoriation, pain in bladder, hematuria INTRA-ARTERIAL ROUTE Used for liver cancer treatment Cannulate hepatic artery; continuous infusion of chemo; may use implanted pump High concentration directly to tumor bed High rate of complication with arterial catheters Chemotherapy agents: 5-FU INTRAPERITONEAL ROUTE Indication: Colon and Ovarian Peritoneal space has much surface area; may not be reached by IV chemo Catheters used: implanted port Chemotherapy agents used: Cisplatin, Taxol Advantages: less systemic side effects Disadvantages: infection, pain. INTRAPLEURAL Seeding of pleura Used as sclerosing agent to stop pleural effusions Injected by physician into chest tube and clamped. Patient changes position 15 min for 1 hour Chemotherapy agents used: Bleomycin, Adriamycin, Talc slurry Side effects: severe pain INTRATHECAL ROUTE Meningeal spread of cancer Prophylaxis in Acute Lymphocytic Leukemia Lumbar Puncture Chemotherapy drugs used: Methotrexate

Never used Vinca Alkaloids (causes immediate death) Side effects minimal; mild headache or nausea Notify physician for neck rigidity or change in level of consciousness

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)

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. Depot or reservoir preparations - parental administration may be prolonged by using insoluble salts or suspensions in non-aqueous vehicles.