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?
Which of the following is a disadvantage of intramuscular injection?
What is a major difference between immediate release oral dosage forms and controlled release dosage forms?
What is one of the advantages of using subcutaneous injection?
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Which of the following is a disadvantage of buccal and sublingual delivery?
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What is one of the primary reasons different dosage forms are used in clinical practice?
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Which of the following is a disadvantage of intravenous administration?
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What is a major advantage of transdermal delivery?
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Which of the following factors may be helpful to decide between use of liquid and solid oral dosage forms?
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What is a major disadvantage of rectal delivery?
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Which of the following oral dosage forms is designed to release the drug at a controlled rate?
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What is the purpose of enteric coating in oral dosage forms?
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Which of the following routes of administration is characterized by the absorption of the drug through the mucous membrane of the cheek?
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What is the primary advantage of transdermal delivery?
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Which of the following oral dosage forms is designed for sublingual delivery?
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What is the primary mechanism by which a partial agonist exerts its effect?
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Which of the following factors contributes to the duration of a drug's effect?
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Which of the following characteristics of acetylcholine leads to its designation as a neurotransmitter?
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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?
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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.