Pharmaceutical Dosage Forms

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Questions and Answers

What is one of the advantages of using the inhalation route of drug administration as in treatment of asthma and chronic obstructive pulmonary disease?

The drug is first metabolized by the liver, reducing its effect

The drug is eliminated more quickly, reducing the risk of overdose

The drug passes directly into the bloodstream, resulting in a rapid effect (correct)

The drug is distributed evenly throughout the body, reducing side effects

Which of the following is a disadvantage of intramuscular injection?

Risk of nerve injury (correct)

Reduced patient anxiety

Rapid onset of action

Increased bioavailability

What is a major difference between immediate release oral dosage forms and controlled release dosage forms?

Controlled release dosage forms reduce fluctuation in drug blood levels. (correct)

Controlled release dosage forms have a faster onset of action.

Controlled release dosage forms have more flexibility in dose adustment.

Controlled release dosage forms typically have a less convenient dosing schedule.

What is one of the advantages of using subcutaneous injection?

Sustained effects Signup and view all the answers

Which of the following is a disadvantage of buccal and sublingual delivery?

It is contraindicated in patients with oral cavity injury. Signup and view all the answers

What is one of the primary reasons different dosage forms are used in clinical practice?

To provide accurate dosing Signup and view all the answers

Which of the following is a disadvantage of intravenous administration?

Removal after inadvertent overdose is more difficult Signup and view all the answers

What is a major advantage of transdermal delivery?

It provides consistent drug levels for extended periods. Signup and view all the answers

Which of the following factors may be helpful to decide between use of liquid and solid oral dosage forms?

Liquid dosage forms often allow for more rapid onset of action Signup and view all the answers

What is a major disadvantage of rectal delivery?

It is contraindicated in patients with immunosuppression or increased risk of bleeding. Signup and view all the answers

Which of the following oral dosage forms is designed to release the drug at a controlled rate?

Sustained-release tablets Signup and view all the answers

What is the purpose of enteric coating in oral dosage forms?

To prevent degradation of the drug in the stomach Signup and view all the answers

Which of the following routes of administration is characterized by the absorption of the drug through the mucous membrane of the cheek?

Buccal Signup and view all the answers

What is the primary advantage of transdermal delivery?

Avoidance of the first pass effect Signup and view all the answers

Which of the following oral dosage forms is designed for sublingual delivery?

Thin Films Signup and view all the answers

What is the primary mechanism by which a partial agonist exerts its effect?

By binding to the same receptor as the endogenous ligand, but with lower efficacy Signup and view all the answers

Which of the following factors contributes to the duration of a drug's effect?

The rate of drug elimination Signup and view all the answers

Which of the following characteristics of acetylcholine leads to its designation as a neurotransmitter?

It is a chemical messenger that signals across a synaptic cleft Signup and view all the answers

A report on drug X has been submitted to the FDA for approval. The report notes that drug X acts on receptor Y to prevent activation of the receptor by other chemicals. Which of the following is the best way to describe the pharmacodynamics of drug X?

Receptor Y antagonist Signup and view all the answers

Study Notes

Solid Oral Dosage Forms

Accurate dose, less bulky, longer beyond use date, more palatable, and special release characteristics
Cons: more specific dosing, easier to swallow, and faster onset of action

Controlled Release Dosage Forms

Pros: less fluctuation in drug blood levels, frequency reduction in dosing, enhanced convenience and compliance, and reduction in adverse side effects
Cons: loss of flexibility in adjusting the dose and inability to manipulate administration

Buccal and Sublingual Delivery

Pros: avoidance of first pass effect and rapid onset of action
Cons: avoidance in patients with oral cavity injury, avoiding eating/drinking until medication dissolves completely

Rectal Delivery

Pros: lower first pass effect than oral administration, alternate oral route if patient is unable to take by mouth
Cons: irregular and unpredictable absorption, embarrassment or discomfort for patient or caregiver, and avoidance in patients with immunosuppression or increased risk of bleeding

Transdermal Delivery

Only a small part of the skin needs to be utilized, can be applied to different areas of the body at each dosing interval, and allows skin to recover
Epidermis of the skin is a barrier to drug absorption, provides slow permeation resulting in consistent drug levels for extended periods

Pulmonary Delivery

Used mostly for local delivery of drugs for asthma and chronic obstructive pulmonary disease
Attributes of the lungs make this route advantageous: large surface area, well supplied with blood vessels, and the drug passes directly into the bloodstream with a rapid effect
The size of particles administered by means of inhalation influences the part of the lung which they reach

Intramuscular Injection

Pros: sustained effects, suspension allows a slow release, and solution allows a rapid release
Cons: inadvertent subcutaneous administration, pain/patient anxiety, risk of nerve injury, and avoidance in patients with increased bleeding tendency

Subcutaneous Injection

[No specific points mentioned]

Intravenous Administration

Pros: can administer drugs destroyed or inactivated in GI tract or with poor bioavailability, and rapid onset of action
Cons: removal after inadvertent overdose is more difficult, more expensive, administration by trained professional, and infection risk

Importance of Dosage Forms

Dosage forms are necessary to provide accurate dosing, convenience of administration, and protect the drug
Dosage forms may control the rate of drug release, mask the taste of the drug, separate incompatible ingredients, etc.

Routes of Drug Administration with Corresponding Dosage Forms

Oral: syrups, elixirs, emulsions, tablets, oral disintegrating tablets, sustained-release tablets, enteric-coated tablets, capsules, softgels
Rectal: creams, ointments, gels, suppositories, aerosol foams, enemas
Vaginal: creams, ointments, gels, suppositories
Topical: creams, ointments, gels, transdermal patches, lotions
Colonic: rectal foams
Otic: aqueous drops, oily drops
Nasal: creams, ointments, gels, drops, sprays, metered-dose sprays
Pulmonary: metered-dose inhalers, dry powder inhalers, capsules for dry powder inhalation, nebulized solutions
Intravenous: aqueous solutions, oily solutions, suspensions
Intramuscular: aqueous solutions, oily solutions, suspensions
Subcutaneous: aqueous solutions, aqueous suspensions

Pharmacology

Innovative drug delivery systems can supply drugs to organs difficult to reach by conventional routes, without causing systemic toxicity.

Drug-Receptor Interactions

Receptors are protein molecules including enzymes, transporters, and ion channels where a ligand (specific endogenous neurotransmitter/hormone or an external pharmacological agent) binds to, resulting in a cellular response.
Orphan Receptors are receptors for which the ligand remains unknown.
Ligand is an ion or molecule that forms a complex with a biomolecule to serve a specific biological purpose.

Endogenous Ligands

Neurotransmitters (NT): chemical messengers signaling across a synaptic cleft, such as Acetylcholine (Ach), Epinephrine (EPI), and Norepinephrine (NE).
Hormones (peptide): secreted from neuroendocrine cells into the blood to signal at distant cells and tissues, such as Aldosterone, Insulin, Nerve growth factor (NGF), and Thyroid hormone (TH).

Pharmacodynamics

A drug is a chemical agent that selectively interacts with specific target molecules (i.e., receptors) to alter their specific physiological functions.
Agonist: a drug that activates receptors to result in either stimulation or inhibition of the function of various types of cells and organs.
Antagonist: a drug that prevents receptor activation by agonists.

Factors Contributing to Drug Effect

Drug dosage: the effect of a drug increases with an increased amount of drug up to the point of receptor saturation.
Number of Receptors: receptors may be differentially expressed in one tissue to the next and, therefore, mediate different levels of biological responses.
Disease states: disease states can affect drug pharmacology.
Drug Efficacy/Intrinsic activity: the ability to activate or block a receptor, which is the maximum effect a drug can produce regardless of the dose.
Drug Potency/Affinity: the rate of drug-receptor binding and drug-receptor release, which is the amount of drug needed to produce a particular effect.

Sub-Disciplines of Pharmacology

Pharmacodynamics: effects and mechanisms of drug action, including drug-receptor interactions, dose-response relationships, and signal transduction.
Pharmacokinetics: movement of a drug throughout the body, including absorption, distribution, metabolism, and excretion.
Pharmacogenetics: genetic factors play a role in the rate of drug metabolism, drug-induced toxicity, and drug-induced allergies.

Drug Administration

Drug treatment requires getting a drug to its specific target site or sites in tissues where the drug has its action.
The process of administration involves introducing the drug into the body, sometimes far from the target site.

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Description

This quiz covers the advantages and disadvantages of solid oral dosage forms and controlled release dosage forms in pharmaceuticals.