2: Routes of Administration

What refers to the direct administration of a drug into the bloodstream?

Intravascular Route

Why does the intravascular route provide a baseline of 100% absorption?

Because it bypasses absorption barriers and the liver entirely.

Which of the following is NOT an intravascular route of administration based on the provided text? A. Intravenous (IV) B. Intra-arterial (IA) C. Intracardiac (IC) D. Intrathecal

D. Intrathecal

The extravascular route guarantees 100% absorption.

False. The correct statement is: Absorption varies and is generally less than 100%.

What refers to the administration where the drug must pass through tissues or membranes before reaching the systemic circulation?

Extravascular Route

What are the four extravascular enteral routes of administration?

Oral (per orem), Rectal, Buccal, Sublingual

What are the three extravascular parenteral routes of administration mentioned in the overview?

Subcutaneous (SC), Intramuscular (IM), Intrathecal

Which extravascular parenteral route is injected into the spinal canal and is highly painful?

Intrathecal

What are the extravascular routes classified under "Others"?

Inhalational (direct to bronchioles), Intranasal, Ocular, Vaginal, Urethral, Transdermal patches

What route involves a drug being injected directly into a peripheral vein?

Intravenous (IV) Route

What classification of the IV route involves a large dose injected completely and immediately?

IV Bolus (IV Push)

True or False. The IV Bolus reaches maximum effect (100%) quickly and maintains its level indefinitely.

False. The correct statement is: Reaches maximum effect (100%) quickly but depletes over time.

Which classification of the IV route is ideal for sudden emergencies (e.g., Epinephrine)?

IV Bolus (IV Push)

What refers to the classification of the IV route where a drug is administered slowly to slowly reach and maintain a steady-state effective concentration?

IV Infusion

What is an ideal use and example for an IV Infusion? A. Sudden emergencies (e.g., Epinephrine) B. Maintenance (e.g., 5% Dextrose) C. Local effect (e.g., laxatives) D. Diagnostic agents

B. Maintenance (e.g., 5% Dextrose)

What are the advantages of the Intravenous (IV) Route?

Offers rapid onset, Guarantees 100% total dose absorption

What are the disadvantages of the Intravenous (IV) Route?

Difficult to administer, Carries a high risk of toxicity, Requires trained nurses, Expensive

What is the lethal consequence of a rapid IV push of Potassium Chloride (KCl)?

Immediate cardiac arrest

True or False. Rapid IV push of Potassium Chloride (KCl) is the safest way to treat hypokalemia.

False. The correct statement is: It must be administered carefully when treating hypokalemia.

What route is administered directly into an artery to achieve a high drug concentration in a specific tissue before systemic distribution occurs?

Intra-arterial (IA) Route

What is the key mechanism of the Intra-arterial (IA) route when delivering fibrinolytics? A. It provides a steady depot effect over time B. It acts as a Beta-1 selective agonist C. Used to target localized areas directly, such as delivering fibrinolytics to a specific blood vessel to lyse (dissolve) stable fibrin clots D. It bypasses the Blood-Brain Barrier (BBB)

C. Used to target localized areas directly, such as delivering fibrinolytics to a specific blood vessel to lyse (dissolve) stable fibrin clots

What are the important examples of the Intra-arterial (IA) Route?

Diagnostic agents, Cancer therapy, Fibrinolytics/Thrombolytics (e.g., Streptokinase)

What route is administered directly into the heart chambers, heart muscles, or ventricles?

Intracardiac (IC) Route

Which of the following acts as a Beta-1 selective agonist to increase both the force of contraction and the rate of contraction? A. Streptokinase B. Dobutamine C. Fentanyl D. Epinephrine

B. Dobutamine

What is the medical term for increasing the force of contraction?

Inotropy

What is the medical term for increasing the rate of contraction?

Chronotropy

What are the important examples for the Intracardiac (IC) route?

Streptokinase, Dobutamine

True or False. The Intracardiac (IC) Route is a crucial route and drug choice during a cardiogenic shock when the heart suddenly fails to pump effectively.

True.

What refers to administration via the oral cavity?

Oral Route (Per Orem)

What are the advantages of the Oral Route?

Most convenient, Cheapest route

What is the typical absorption yield of the Oral Route? A. 100% absorption B. ~80-90% absorption C. ~50-60% absorption D. ~10% absorption

C. ~50-60% absorption

What are the two main disadvantages of the Oral Route?

Inefficient (yielding only ~50-60% absorption), Subject to the First-Pass Effect, which significantly reduces systemic bioavailability

For which patient populations is the Oral Route contraindicated?

Babies, Unconscious patients, Stroke patients, Patients having an active epileptic attack

True or The oral route often requires formulation with masking agents to hide bitter tastes.

True.

What is the rapid uptake and metabolism of an orally administered drug into an inactive compound before it can reach systemic circulation?

First-Pass Effect

Which organ exclusively mediates the First-Pass Effect?

The liver

Into what type of compound does the liver metabolize the drug ready for excretion?

More polar, Hydrophilic, Inactive compound

The First-Pass Effect heavily reduces the drug's 100% bioavailability.

True.

What route uses tablets that are placed in the gums/cheek pouch (buccal sulcus)?

Buccal Route

What route uses tablets that are placed under the tongue?

Sublingual Route

What are the advantages of the Buccal and Sublingual Routes?

Rapid absorption due to highly vascularized tissues, Minimal first-pass effect (~10%) compared to oral ingestion, Excellent drug stability

What is the typical first-pass effect percentage exhibited by the buccal and sublingual routes? A. 100% B. ~50-60% C. ~10% D. ~80-90%

C. ~10%

What is the required dissolution time for a sublingual tablet?

Dissolves in <30 mins

What is the required dissolution time for a buccal tablet?

Takes 1–2 hours

What are the disadvantages of the Buccal and Sublingual routes?

Inconvenient, Limited to small doses

What are the important examples of the Sublingual route?

Sublingual Nitroglycerin, Sublingual Clonidine (Catapres)

What route involves administration into the rectum via suppositories?

Rectal Route

What is the estimated absorption yield of the Rectal Route due to bypassing the liver? A. ~50-60% absorption B. ~80-90% absorption C. 100% absorption D. ~10% absorption

B. ~80-90% absorption

The Rectal Route is strictly for local effects (e.g., laxatives).

False. The correct statement is: Can exert both local (e.g., laxatives) and systemic effects.

Which route is highly useful for pediatric patients who cannot swallow pills?

Rectal Route

What are the disadvantages of the Rectal Route?

Erratic/variable absorption, Low patient acceptability, Difficult administration

What instructions should be given to patients to minimize pain before inserting a suppository?

Raise one foot, Lean forward, Slightly wet/moisten the suppository before insertion

What route is administered into the fat layer under the skin?

Subcutaneous (SC) Route

What are the common sites for Subcutaneous (SC) administration?

Upper arm, Abdomen, Front of thigh

What are the advantages of the Subcutaneous (SC) Route?

Allows for self-administration, Complete absorption

What are the important examples for the Subcutaneous (SC) Route?

Insulin, Heparin

What are the disadvantages of the Subcutaneous (SC) Route?

Painful due to high nerve density, Tissue damage, Limited to small doses (~2 mL)

What refers to cell death and bulging of fat tissue caused if injected repeatedly in the exact same spot?

Lipodystrophy

What counseling point must be given to patients regarding the Subcutaneous (SC) Route to avoid lipodystrophy?

Patients must rotate injection sites.

What route is administered deep into the muscles?

Intramuscular (IM) Route

What are the target muscles for the Intramuscular (IM) route?

Deltoid, Gluteus maximus, Vastus lateralis

Which of the following is NOT an advantage of the Intramuscular (IM) Route? A. Larger volume B. Exhibits a Depot Effect (sustained release) C. Easier to administer than IV D. Painless due to low nerve density

D. Painless due to low nerve density

What refers to the sustained release where the drug settles in the muscle and is released slowly into the bloodstream over time, providing a prolonged duration of action?

Depot Effect

True or False. The Intramuscular (IM) route requires trained personnel and can be painful.

True.

T or F. Under new responsibilities, trained pharmacists are now authorized as immunizers for specific IM vaccines.

True.

What are the important examples of specific IM vaccines?

Influenza, Pneumococcal, Cervical vaccines

What route uses drugs formulated as liquid droplets, solid particles, or aerosols inhaled directly into the pulmonary tract?

Inhalational Route

What specific parts of the pulmonary tract does the inhalational route target?

Bronchioles, Alveoli

What are the advantages of the Inhalational Route?

Features highly rapid absorption, Bypasses the liver entirely (no first-pass effect)

What are the important examples of drugs administered via the Inhalational Route?

Asthma medications, Inhalational anesthetics (e.g., Sevoflurane, Isoflurane)

True or False.Due to the cough reflex, some drugs administered via the inhalational route may be swallowed.

True.

Through what devices does the inhalational route deliver drugs rapidly to the Central Nervous System (CNS) and respiratory tissues?

Inhalers, Rota-halers, Inhalational anesthetics

True or False. Dosing via the inhalational route is exact and does not require preparation.

False. The correct statement is: Dosing is not exact. Devices require priming to ensure the patient receives a full 100% dose.

What is the process of spraying the first dose into the air to ensure the patient receives a full 100% dose upon inhalation?

Priming

What technique should patients be instructed to use when handling an inhaler? A. Place the inhaler directly against the lips B. Use an open-mouth technique (holding the inhaler 1 to 2 inches away) C. Inhale through the nose while pressing the device D. Swallow immediately after spraying

B. Use an open-mouth technique (holding the inhaler 1 to 2 inches away)

What are the primary diseases/uses for inhaler administration and devices?

COPD, Asthma, Inhalational anesthetics

What device is highly recommended when using inhalers containing corticosteroids?

A spacer

What are the two components of Seretide?

Salmeterol (a LABA), Fluticasone (a corticosteroid)

What condition can be caused by improper inhalation of corticosteroids because they act locally as immunosuppressants?

Oral candidiasis (fungal infection in the mouth)

What should patients do to prevent oral candidiasis after using corticosteroid inhalers?

Use a spacer, Spit/rinse their mouth after use

What route involves applying drugs directly to body surfaces for a strictly local effect?

Topical Route

True or False. If the skin is broken, topical drugs cannot be absorbed into systemic circulation.

False. The correct statement is: If the skin is broken, topical drugs can be inadvertently absorbed into systemic circulation, leading to side effects like redness or toxicity.

What are the important examples of the Topical Route?

Eye (ophthalmic) and ear (otic) drops, Antiseptics, Sunscreens, Lotions, Callous removal, Antibacterial ointments, Local anesthetics

What route is applied to the skin specifically designed for systemic absorption?

Transdermal Route

True or False.Compared to IV administration, the transdermal route provides non-invasive, targeted systemic delivery.

True.

What characteristics must the active drug have to successfully pass through the skin layers into the bloodstream via the transdermal route?

Low-dose, Low-molecular-weight

Which of the following are examples of 1st Generation transdermal classifications? A. Scopolamine and Fentanyl B. Nitroglycerin and Nicotine patches C. Clonidine (hypertension) and Estrogen (hormone therapy/oral contraceptives) D. Improved overall delivery systems

C. Clonidine (hypertension) and Estrogen (hormone therapy/oral contraceptives)

What classification of the Transdermal Route features improved overall delivery systems?

2nd Generation

What classification of the Transdermal Route utilizes novel technology to increase the scope of targetable molecules?

3rd Generation

What are the components that make up the anatomy of a transdermal patch?

Drug reservoir, Occlusive baseplate, Impermeable plastic backing, Absorbent pad

What are the important examples of small lipid-soluble molecules used in the transdermal route?

Nitroglycerin (vasodilator for heart conditions), Nicotine patches, Scopolamine (motion sickness), Fentanyl (pain management), Steroid patches

What route is administered directly into the nasal cavity?

Intranasal Route

What are the primary uses of the Intranasal Route?

Nasal decongestants, Anti-tussives

What drugs can be delivered systemically using the Intranasal Route?

Propranolol, Low-dose hormones

What route is injected just beneath the dermis, typically forming a "bleb" or wheal on the skin surface?

Intradermal (ID) Route

The Intradermal (ID) Route is known to be painless.

False. The correct statement is: Known to be extremely painful.

What is the most common application of the Intradermal (ID) Route?

Allergy testing

What route is injected directly into the joint space (the layer between the bones)?

Intra-articular Route

What are the functions of the Intra-articular Route?

Replaces lost synovial fluid, Directly reduces joint inflammation

True or False. In Rheumatoid Arthritis (RA), the protective hyaluronic acid layer disappears, causing severe bone friction and pain.

True.