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Questions and Answers
What is the primary benefit of adding adrenaline to local anaesthetic?
What is the primary benefit of adding adrenaline to local anaesthetic?
Which insulin formulation provides basal insulin levels with once daily dosing?
Which insulin formulation provides basal insulin levels with once daily dosing?
What is Nusinersen primarily used for?
What is Nusinersen primarily used for?
Which method is used for the administration of Ranibizumab?
Which method is used for the administration of Ranibizumab?
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Which of the following drugs is administered intrathecally?
Which of the following drugs is administered intrathecally?
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What is the effect of esterification of steroid hormones when injected in oily solutions?
What is the effect of esterification of steroid hormones when injected in oily solutions?
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What is the primary function of Aflibercept in treatments?
What is the primary function of Aflibercept in treatments?
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What determines the absorption rate of a subcutaneous implant of steroid hormones?
What determines the absorption rate of a subcutaneous implant of steroid hormones?
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Which of the following conditions can be treated with intravitreal implants?
Which of the following conditions can be treated with intravitreal implants?
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Aminoglycosides can be used intrathecally for what purpose?
Aminoglycosides can be used intrathecally for what purpose?
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Which route of administration is NOT typically associated with absorption through the gastrointestinal tract?
Which route of administration is NOT typically associated with absorption through the gastrointestinal tract?
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What primarily influences the absorption rate of a drug taken orally?
What primarily influences the absorption rate of a drug taken orally?
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Which drug absorption mechanism is most likely to involve carrier-mediated transport?
Which drug absorption mechanism is most likely to involve carrier-mediated transport?
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Which of the following drugs is an example of one that is absorbed sublingually?
Which of the following drugs is an example of one that is absorbed sublingually?
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What is a common characteristic of drugs that are poorly absorbed through the gastrointestinal tract?
What is a common characteristic of drugs that are poorly absorbed through the gastrointestinal tract?
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Which factor is NOT listed as influencing drug absorption?
Which factor is NOT listed as influencing drug absorption?
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What percentage of orally administered drugs are typically absorbed within 1-3 hours?
What percentage of orally administered drugs are typically absorbed within 1-3 hours?
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Which of the following drug absorption routes involves application to epithelial surfaces?
Which of the following drug absorption routes involves application to epithelial surfaces?
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What does AUC stand for in the context of drug exposure?
What does AUC stand for in the context of drug exposure?
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Which of the following factors does NOT influence bioavailability?
Which of the following factors does NOT influence bioavailability?
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What is the primary purpose of sublingual administration?
What is the primary purpose of sublingual administration?
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Why might rectal administration be preferred for certain patients?
Why might rectal administration be preferred for certain patients?
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What is a consequence of the first-pass metabolism?
What is a consequence of the first-pass metabolism?
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What effect does rate of absorption have on drug administration?
What effect does rate of absorption have on drug administration?
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How does buccal administration compare to intravenous administration in emergency settings?
How does buccal administration compare to intravenous administration in emergency settings?
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What is a common misconception about drugs absorbed from the oral cavity?
What is a common misconception about drugs absorbed from the oral cavity?
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What is the advantage of chemical modification of drugs like Ipratropium?
What is the advantage of chemical modification of drugs like Ipratropium?
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Which method of drug administration produces the fastest onset of action?
Which method of drug administration produces the fastest onset of action?
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Which factor can directly impair drug absorption due to a decrease in GI motility?
Which factor can directly impair drug absorption due to a decrease in GI motility?
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What is the primary goal of modified-release drug formulations?
What is the primary goal of modified-release drug formulations?
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What happens to peak tissue concentration when using intravenous infusion as opposed to bolus injection?
What happens to peak tissue concentration when using intravenous infusion as opposed to bolus injection?
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How does particle size affect drug absorption?
How does particle size affect drug absorption?
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Which factor limits drug absorption when administered subcutaneously or intramuscularly?
Which factor limits drug absorption when administered subcutaneously or intramuscularly?
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How does increased local blood flow affect drug absorption?
How does increased local blood flow affect drug absorption?
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Which of the following conditions is least likely to reduce splanchnic blood flow?
Which of the following conditions is least likely to reduce splanchnic blood flow?
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Which drug is specifically intended for a local effect in the gut?
Which drug is specifically intended for a local effect in the gut?
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What does bioavailability (F) represent in pharmacology?
What does bioavailability (F) represent in pharmacology?
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What effect does diarrhea have on drug absorption?
What effect does diarrhea have on drug absorption?
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Which of the following correctly describes the role of muscarinic receptor blockers in GI motility?
Which of the following correctly describes the role of muscarinic receptor blockers in GI motility?
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Flashcards
Routes of Administration
Routes of Administration
Different ways to deliver a drug to the body, such as oral or injection.
Oral Administration
Oral Administration
Taking drugs by mouth; absorption begins in the small intestine.
Sublingual/Buccal Route
Sublingual/Buccal Route
Drugs absorbed directly via oral mucosa under the tongue or inside the cheeks.
Intravenous Injection
Intravenous Injection
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Drug Ionization
Drug Ionization
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Carrier-Mediated Transport
Carrier-Mediated Transport
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Absorption Rate
Absorption Rate
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Factors Influencing Absorption
Factors Influencing Absorption
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AUC (Area Under the Curve)
AUC (Area Under the Curve)
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Bioavailability (F)
Bioavailability (F)
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Factors affecting Bioavailability
Factors affecting Bioavailability
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Peak Plasma Concentration
Peak Plasma Concentration
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Sublingual administration
Sublingual administration
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Buccal administration
Buccal administration
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GI Motility
GI Motility
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Rectal administration
Rectal administration
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Local vs. Systemic Effects
Local vs. Systemic Effects
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Splanchnic Blood Flow
Splanchnic Blood Flow
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T max and C max
T max and C max
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Gastric Stasis
Gastric Stasis
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Modified-Release Preparations
Modified-Release Preparations
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Absorption Factors
Absorption Factors
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First-pass Metabolism
First-pass Metabolism
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Beclomethasone
Beclomethasone
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Bronchodilators
Bronchodilators
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Hyaluronidase
Hyaluronidase
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Factors affecting absorption
Factors affecting absorption
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Prolonged Absorption
Prolonged Absorption
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Adrenaline in Anaesthetics
Adrenaline in Anaesthetics
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Long-Acting Insulin
Long-Acting Insulin
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Intrathecal Administration
Intrathecal Administration
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Subcutaneous Implantation
Subcutaneous Implantation
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Nusinersen
Nusinersen
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Ranibizumab
Ranibizumab
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Aflibercept
Aflibercept
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Intravitreal Injection
Intravitreal Injection
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Intravitreal Implants
Intravitreal Implants
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Study Notes
Absorption Routes of Administration
- Different ways a drug can be administered:
- Oral (sublingual or buccal, rectal)
- Application to other epithelial surfaces (skin, vagina, nasal mucosa)
- Inhalation
- Injection (subcutaneous, intramuscular, intravenous, intrathecal, intravitreal)
Oral Administration
- Most small drugs are taken orally.
- Absorption begins in the small intestine.
- Non-polar drugs are absorbed directly in the mouth (e.g., buccal mucosa).
- Examples include organic nitrates, buprenorphine
- Peptides and proteins are digested in the GI tract.
- Not suitable for biopharmaceuticals.
- Drug absorption occurs via passive transfer across epithelial barriers.
- Absorption rate is determined by drug ionization and lipid solubility.
- Strong acids and bases cannot be absorbed by the GI tract because they are fully ionized.
- Intestinal drug absorption can involve carrier-mediated transport.
- Levodopa uses a carrier for phenylalanine.
- Fluorouracil uses a carrier for pyrimidines (thymine & uracil).
- Iron absorption is via specific carriers in the jejunal mucosa.
- Calcium absorption is facilitated by vitamin D-dependent carrier.
Factors Affecting GI Absorption
- 75% of orally administered drugs are absorbed within 1-3 hours.
- Factors influencing drug absorption:
- Gut content (fed vs. fasted)
- GI motility
- Splanchnic blood flow
- Physiochemical factors & drug-drug interactions
- Genetic polymorphisms and/or drug competition for transporters
- Feeding affects gut content and splanchnic blood flow, influencing Tmax and Cmax.
- GI motility impacts absorption.
- Disorders like migraine and diabetic neuropathy can slow absorption due to gastric stasis.
- Muscarinic receptor blockers reduce motility (e.g. Metoclopramide increases motility to increase absorption)
- Diarrhoea can impair drug absorption.
- Splanchnic flow can be reduced by exercise, hypovolemia, or heart failure.
- Particle size (e.g. Digoxin plasma concentrations varied due to different formulations).
- Therapeutic drug formations aim to achieve desired characteristics like capsule/tablet formulations, release at the desired rate, some drugs for local effect.
Bioavailability and Bioequivalence
- Oral drugs must penetrate the intestinal mucosa and survive presystemic/first-pass metabolism.
- Bioavailability (F) indicates the fraction of orally administered dose reaching systemic circulation as intact drug.
- F takes into account both absorption and local metabolic degradation.
- Measurement of F involves comparing plasma drug concentration vs time curves after oral vs. intravenous administration.
- AUC (area under the curve) provides an integrated measure of drug exposure.
- F is estimated as AUC oral/AUC intravenous.
- Bioavailability is influenced by enzyme activity in the gut wall or liver, gastric pH, intestinal motility.
- Bioavailability varies among individuals under differing conditions and reflects the total drug reaching systemic circulation, not the rate of absorption.
- Rate of absorption affects peak plasma concentration and drug effect
Sublingual or Buccal Administration
- Absorption from the oral cavity is useful for rapid response and rapidly metabolized drugs.
- Examples of sublingual administration include glyceryl trinitrate and buprenorphine.
- Buccal midazolam is effective for terminating early status epilepticus in children.
Rectal Administration
- Rectal administration is mainly used for local and systemic effects.
- Examples include mesalazine suppositories/enemas for ulcerative colitis.
- Absorption can be rapid and more complete than oral.
- Rectal administration may be unreliable.
- Only a fraction of the drug enters systemic circulation.
- Useful for patients unable to take medication orally (e.g., vomiting, post-surgery, palliative surgery).
Cutaneous Administration
- Used for local skin effects (like ibuprofen) and systemic effects.
- Absorption through unbroken skin is poor for most drugs.
- Some substances (e.g., organophosphate insecticides) are well-absorbed and can cause poisoning.
- Examples include nicotine patches, oestrogen/testosterone patches, and fentanyl patches.
Nasal Sprays and Eye Drops
- Nasal sprays and eye-drops use mucosa as delivery routes.
- Peptide hormone analogues are administered as nasal sprays (e.g., antidiuretic hormone, gonadotrophin-releasing hormone, and calcitonin).
- Absorption occurs through mucosa overlying nasal-associated lymphoid tissue (similar to absorption through mucosa overlying Peyer's patches in the small intestine).
Administration by Inhalation
- Used for volatile and gaseous anaesthetics, and drugs affecting the lungs.
- Lung serves as the route of administration and elimination – rapid exchange due to large surface area and rapid blood flow.
- Drugs administered as an aerosol mist of liquid droplets or solid particles (e.g. glucocorticoids and bronchodilators).
- Objective: to achieve high local concentrations in the lung while minimizing systemic effects
Administration by Injection
- Intravenous injection: the fastest and most certain route, giving rapid, high drug concentrations, initially in the right heart and pulmonary vessels, then in systemic circulation.
- Intravenous infusion avoids uncertainties about absorption from other sites and prevents high peak plasma drug concentrations.
- Subcutaneous and intramuscular injections result in a slower effect than oral administration, and absorption depends on the injection site and local blood flow, with faster absorption occurring in areas of higher blood flow.
Why Delay Absorption?
- Delaying absorption is desirable or useful in producing local effects or prolonging systemic absorption.
- Local anaesthetic absorption can be reduced by adding adrenaline.
- The use of protamine and zinc in insulin formulations produces a long-acting insulin form.
- Longer-acting insulin analogues (glargine, detemir, and degladec) provide basal insulin levels over an extended period with a single dose, rather than several injections daily.
Intrathecal Injection
- Used in specialized cases like methotrexate for childhood leukemia (to prevent CNS relapse), local anaesthetics, opioid analgesics, baclofen (for muscle spasms), antibiotics and more.
Intravitreal Injection
- Intravitreal injections use monoclonial antibodies to target vascular endothelial growth factor (VEGF) for treatment of age-related macular degeneration and macular oedema.
- Intravitreal fusion proteins, like aflibercept, also target VEGF.
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Description
Explore the various methods of drug administration through this quiz. From oral to injection, learn how different routes affect drug absorption and the factors influencing the rates of absorption. Perfect for students studying pharmacology or related fields.