Subject: Pharmacology Lab Topic: Conference for Experiment Lecturer: Dra.

Dela Cruz Date of Lecture: July 2, 2011 Transcriptionist: Madame and Super Minions Pages:5

EXPERIMENT 1 Onset and Duration of Drug Effect in Relation to Route of Drug Administration in Rabbits

Animal : One (1) rabbit per ten (10) students Materials : One (1) tuberculin syringe (without needle) Four (4) tuberculin syringe with g 25 needle One (1) 2.5 cc syringe (without needle) One (1) tongue depressor Cotton balls Alcohol Distilled water Thiopental Sodium Solution 2.0 % (0.02 mg/g) *For the procedures please refer to your manual pages 110-112 How to compute for the dose of Thiopental Sodium? 1. To compute for the amount(dose) of Thiopental needed use the formula: Dose of Drug = Weight of the rabbit x Concentration of the drug So for the experiment, given the concentration of the drug=0.02 mg/g and the weight of the rabbit = 570g Dose of the drug = 570g x 0.02mg/g = 11.4 mg of Thiopental Sodium 2. Since Thiopental Sodium is in liquid form, we have to convert it to ml using ratio and proportion. Ex. 11.4mg of Thiopental = 20 mg Z 1ml Z = (11.4 mg)(1ml)/(20 mg) Z = 0.57 ml **20 mg/ml came from the Thiopental Sodium solution given in the experiment. Since 2.0% yung solution, each ml of the solution contains 20 mg Thiopental ( It was assumed na nung gnawa yung drug, 20 mg was dissolved in 1000 ml of water kaya naging 20mg/1000ml = 0.02 = 2.0%. Getching??

Period of Observation Oral - note the time of administration and observe every 10-15 min. Intravenous - time of administration and every 1-2 min. thereafter Intramuscular - time of administration and every 5 min. thereafter Intraperitoneal - time of administration and every 2-5 min. thereafter Subcutaneous - time of administration and every 5-10 min. thereafter DISCUSSIONS THIOPENTAL SODIUM -A barbiturate and general anesthetic 1

SY 2011-2012

-One-arm circulation -Normal dose in humans is 20-50 mg/kg/dose -Expected result is sleepiness or relaxation
NICE-TO-KNOW about the characteristics of Thiopental Sodium From Goodman and Gilman Thiopental sodium is administered intravenously. It may be injected either as a single bolus, intermittently, or as a continuous infusion. The use of a continuous infusion increases the likelihood of overdosage, with a subsequent prolonged recovery period. For single or intermittent injections of thiopental sodium, the concentration employed should not exceed 2.5% in aqueous solution. Injections are most safely made into the side port of a flowing intravenous infusion of saline solution or 5% dextrose in water. If concentrations greater than 2.5% are injected extravascularly, the pain may be severe, and tissue necrosis can occur. Of even greater concern are the results of inadvertent intraarterial injection of concentrated solutions of thiopental. The arterial endothelium and deeper layers are immediately damaged and endarteritis follows, often with thrombosis exacerbated by subsequent arteriolar spasm. Vascular ischemia and even gangrene may result. For induction of anesthesia in an adult patient, the usual procedure is to inject a 50-mg test dose moderately rapidly, observe the response, and then inject an additional dose of 100 to 200 mg over 20 seconds. In a muscular, robust individual, as much as 500 mg occasionally may be necessary to induce general anesthesia. If the dose is injected too slowly, a stage of excitement may be encountered. Such excitatory movements are more common with methohexital. Conversely, if too much drug is injected too rapidly, profound anesthesia may supervene with apnea and hypotension. The usual response after a correctly chosen and administered dose is for the patient to experience a faint taste of garlic, followed by a suppressed yawn and then the smooth, rapid appearance of sleep. There is an initial and transient period of relaxation, which may be appropriate for very short procedures such as correction of a dislocation, and the airway may become impaired by the in folding of soft tissues around the tongue and pharynx. Recovery following thiopental should be characterized by smooth, rapid awakening to consciousness. However, if there is postoperative pain, restlessness may become evident and analgesics should be given (an antianalgesic effect of thiopental at low circulating concentrations may be partially responsible for this response). Shivering often occurs postoperatively as heat is generated to restore body temperature that has decreased during anesthesia and surgery. Postural hypotension may be encountered, and patients should not be moved too hurriedly.

RIGHTING REFLEX  The parameter used in the experiment; also called the static reflex  Any of the various righting reflex which tend to bring the body into normal position and space and resist forces acting to displace it out of the normal position ** The effect of the drug is the force that displaced the animal

ROUTES OF ADMINISTRATION
I. ORAL showed a markedly slow response the drug did not induce an expected onset which is to lose the righting reflex this means that the drug did not take full effect because it was not efficiently absorbed the drug is susceptible to the first pass effect due to the combined action of the epithelial cell secretions of the GIT and the hepatic drug metabolizing enzyme to degrade or inactivate the drug. When this happens, the bioavailability of the drug is lessened, thus lessened effectivity ADVANTAGES: 1. most convenient, safest, ease of administration, cheaper DISADVANTAGES: 1. first pass effect (metabolized in the liver, lungs and GIT) 2. surface area (increase surface area will increase absorption) 3. weakly acidic drugs are absorbed more easily than weak bases 4. nonionized (lipophilic) drugs is absorbed easily than ionized drugs 5. can irritate the digestive tract.

II. INTRAVENOUS -Route that has the fastest onset of effect - High bioavailability because it goes straight into the systemic blood stream by passing the first pass effect

-Takes effect directly on target organs -Large volume may cause the blood vessel to burst. ADVANTAGES: 1. For emergency use 2. Permits dosage titration 3. Suitable for large volume of drugs ( but not that large kasi may possibility na it will burst! If you want for large volume, use IM) DISADVANTAGES: 1. No taking it back!!! (once na naturok mo na wala ka ng magagawa kaya ingat lagi. Always monitor your patient) 2. May cause unfavorable reactions like allergies and anaphylaxis 3. Difficult to administer 4. Inject slowly 5. Not suitable for oily solutions or insoluble substances 6. Pain 7. Expensive III. INTRAMUSCULAR -Used to administer large volumes of drug -Slower effect than IV because muscles are not highly vascular -Easier to inject -Slower onset because muscle serve depot -DISADVANTAGE: Thiopental is irritating to the muscle -Absorption rate may vary maybe due to blood flow, heat, or massage Example: If an injection was made at Vastus Lateralis, its absorption will increase if the patient climbs stairs due to increase in blood flow If you massage the site of injection, there will be an increase in absorption due to increase in blood flow -SPECIAL USE: Suitable for moderate to large volumes; and for oily substances IV. INTRAPERITONEAL -Longer duration of effects compared to IV -Shorter onset compared to oral V. SUBCUTANEOUS -Longer duration of effects compared to IV -Shorter onset compared to oral -Uses: Skin testing For insoluble substances or suspension Implantations of solid pellets -Onset depends on type of drug (e.g. aqueous solution)

Answers to Questions_________________________________________________________________________ 1. Differentiate between enteral and parenteral routes of drug administration. Enteral route of administration means administering the drug through the gastrointerinal tract. While Parenteral route of administration means administering drugs near the vascular vessels or directly on the blood vessel.

2. Enumerate the advantages and disadvantages of the different route of administration. Route
Oral y y y y

Advantages
Most convenient Usually least expensive Safe, does not break skin barrier Administration usually does not cause stress y y y

Disadvantages
Inappropriate for patients with nausea and vomiting Drug may have unpleasant taste or odor Inappropriate when gastrointestinal tract has reduced motility Inappropriate if patient

y y y Sublingual y y y Same as oral route, plus Drug can be administered for local effect More potent than oral route because drug directly enters the blood and bypasses the liver Same as sublingual Can be used when drug has objectionable taste or odor Drug released at slow, steady rate Provides a local therapeutic effect Provides a local effect Few side effects y y

cannot swallow or is unconscious Cannot be used before certain diagnostic tests or surgical procedures Drug may discolor teeth, harm tooth enamel Drug may irritate gastric mucosa Drug can be aspirated by seriously ill patients If swallowed, drug may be inactivated by gastric juice Drug must remain under tongue until dissolved and absorbed Drug is rapidly absorbed into the bloodstream Same as sublingual Dose absorbed is unpredictable

Buccal Rectal

y y y

y y

Vaginal Topical

y y y

y y y

Limited use Maybe be messy and may soil clothes Drug can enter body through abrasions and cause systemic effects Leaves residue on the skin that may soil clothes

Transdermal

y y y y

Subcutaneous

Prolonged systemic effect Few side effects Avoids gastrointestinal absorption problems Onset of drug action faster than oral

y y y y y y y

Intramuscular

y y y y

Intradermal

Pain from irritating drugs is minimized Can administer larger volume than subcutaneous Drug is rapidly absorbed Absorption is slow (this is an advantage in testing for allergies) Rapid effect

Must involve sterile technique because breaks skin barrier More expensive than oral Can administer only small volume Slower than intramuscular administration Some drugs can irritate tissues and cause pain Can produce anxiety reaks skin barrier Can produce anxiety

y y y y

Intravenous

Inhalation

y y y

Introduces drug throughout respiratory tract Rapid localized relief Drug can be administered to unconscious client

Amount of drug administered must be small reaks skin barrier Limited to highly soluble drugs Drug distribution inhibited by poor circulation Drug intended for localized effect can have systemic effect Of use only for the respiratory system

3. Explain the different types of drug formulations. Drug formulation is defined as the process by which different dugs are brought in together for manufacturing a medicinal product. The formulation process of drugs involves inspection of different drugs. During the inspection of the drugs several factors such as solubility of the drugs, the particle size of the drugs, polymorphism and pH are given due consideration since it can have a significant effect on the action of the drug. Types of drug formulation includes: 1. Oral Formulation: Oral formulation of drugs involves formulating drugs in to capsules and tablet form. Drug formulated in a tablet is mainly made from compressing 5-10% of actual drug, glidants, lubricants (80%), disintegrants, binders and 10% of compounds that helps easy disintegration and disaggregation of the tablet in the stomach. In the capsules manufactured this way, the prime active ingredient is enclosed within a gelatinous envelope. The capsule is designed in such a way that the active ingredients of the capsule remain intact for a considerable period of time after ingesting the capsule and delaying the absorption process. 2. Topical medication form: Topical medication form includes formulating drugs in different forms such as ointments, pastes, creams, powder and gel forms.

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