Pharmacology: Absorption Routes of Administration
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Questions and Answers

What is the primary benefit of adding adrenaline to local anaesthetic?

  • Decreases the duration of anaesthesia
  • Reduces absorption, prolonging the anaesthetic effect (correct)
  • Increases pain sensitivity
  • Enhances systemic absorption
  • Which insulin formulation provides basal insulin levels with once daily dosing?

  • Insulin detemir (correct)
  • Regular insulin
  • Insulin lispro
  • Insulin aspart
  • What is Nusinersen primarily used for?

  • Combating cerebral infections
  • Treatment of spinal muscular atrophy (correct)
  • Treatment of wet age-related muscular degeneration
  • Management of muscular oedema
  • Which method is used for the administration of Ranibizumab?

    <p>Intravitreal injection (C)</p> Signup and view all the answers

    Which of the following drugs is administered intrathecally?

    <p>Baclofen (C)</p> Signup and view all the answers

    What is the effect of esterification of steroid hormones when injected in oily solutions?

    <p>Slows absorption (B)</p> Signup and view all the answers

    What is the primary function of Aflibercept in treatments?

    <p>Inhibits vascular endothelial growth factor (C)</p> Signup and view all the answers

    What determines the absorption rate of a subcutaneous implant of steroid hormones?

    <p>Surface area of the implant (D)</p> Signup and view all the answers

    Which of the following conditions can be treated with intravitreal implants?

    <p>Muscular oedema management (A)</p> Signup and view all the answers

    Aminoglycosides can be used intrathecally for what purpose?

    <p>For nervous system infections resistant to antibiotics (B)</p> Signup and view all the answers

    Which route of administration is NOT typically associated with absorption through the gastrointestinal tract?

    <p>Intravenous (A)</p> Signup and view all the answers

    What primarily influences the absorption rate of a drug taken orally?

    <p>The drug's ionization and lipid solubility (C)</p> Signup and view all the answers

    Which drug absorption mechanism is most likely to involve carrier-mediated transport?

    <p>Active transport (C)</p> Signup and view all the answers

    Which of the following drugs is an example of one that is absorbed sublingually?

    <p>Buprenorphine (D)</p> Signup and view all the answers

    What is a common characteristic of drugs that are poorly absorbed through the gastrointestinal tract?

    <p>Strongly acidic or basic drugs (B)</p> Signup and view all the answers

    Which factor is NOT listed as influencing drug absorption?

    <p>Drug's molecular weight (C)</p> Signup and view all the answers

    What percentage of orally administered drugs are typically absorbed within 1-3 hours?

    <p>75% (C)</p> Signup and view all the answers

    Which of the following drug absorption routes involves application to epithelial surfaces?

    <p>Rectal (B)</p> Signup and view all the answers

    What does AUC stand for in the context of drug exposure?

    <p>Area Under Curve (C)</p> Signup and view all the answers

    Which of the following factors does NOT influence bioavailability?

    <p>Blood pressure (A)</p> Signup and view all the answers

    What is the primary purpose of sublingual administration?

    <p>For rapid response (C)</p> Signup and view all the answers

    Why might rectal administration be preferred for certain patients?

    <p>It is useful for patients unable to take medication orally. (C)</p> Signup and view all the answers

    What is a consequence of the first-pass metabolism?

    <p>Reduces the amount of drug reaching systemic circulation. (B)</p> Signup and view all the answers

    What effect does rate of absorption have on drug administration?

    <p>It influences peak plasma concentration. (C)</p> Signup and view all the answers

    How does buccal administration compare to intravenous administration in emergency settings?

    <p>It is easier to administer and can reduce time to drug action. (C)</p> Signup and view all the answers

    What is a common misconception about drugs absorbed from the oral cavity?

    <p>They undergo extensive first-pass metabolism. (C)</p> Signup and view all the answers

    What is the advantage of chemical modification of drugs like Ipratropium?

    <p>To reduce systemic adverse effects (B)</p> Signup and view all the answers

    Which method of drug administration produces the fastest onset of action?

    <p>Intravenous bolus injection (C)</p> Signup and view all the answers

    Which factor can directly impair drug absorption due to a decrease in GI motility?

    <p>Gastric stasis due to disorders (D)</p> Signup and view all the answers

    What is the primary goal of modified-release drug formulations?

    <p>To achieve desired absorption characteristics and reduce dosing frequency (C)</p> Signup and view all the answers

    What happens to peak tissue concentration when using intravenous infusion as opposed to bolus injection?

    <p>It is lower and more stable with infusion (C)</p> Signup and view all the answers

    How does particle size affect drug absorption?

    <p>Variations in particle size can lead to different plasma concentration outcomes (B)</p> Signup and view all the answers

    Which factor limits drug absorption when administered subcutaneously or intramuscularly?

    <p>Diffusion through tissue (C)</p> Signup and view all the answers

    How does increased local blood flow affect drug absorption?

    <p>It enhances absorption (D)</p> Signup and view all the answers

    Which of the following conditions is least likely to reduce splanchnic blood flow?

    <p>Hydration from increased fluid intake (C)</p> Signup and view all the answers

    Which drug is specifically intended for a local effect in the gut?

    <p>Vancomycin (A), Olsalazine (D)</p> Signup and view all the answers

    What does bioavailability (F) represent in pharmacology?

    <p>The fraction of an orally administered dose reaching systemic circulation as unchanged drug (B)</p> Signup and view all the answers

    What effect does diarrhea have on drug absorption?

    <p>Impairs absorption of many oral medications (A)</p> Signup and view all the answers

    Which of the following correctly describes the role of muscarinic receptor blockers in GI motility?

    <p>They can reduce GI motility, complicating drug absorption. (C)</p> Signup and view all the answers

    Flashcards

    Routes of Administration

    Different ways to deliver a drug to the body, such as oral or injection.

    Oral Administration

    Taking drugs by mouth; absorption begins in the small intestine.

    Sublingual/Buccal Route

    Drugs absorbed directly via oral mucosa under the tongue or inside the cheeks.

    Intravenous Injection

    Delivery of drugs directly into the bloodstream via a vein.

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    Drug Ionization

    The degree to which a drug is ionized affects its absorption in the GI tract.

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    Carrier-Mediated Transport

    Absorption process where specific carriers help transport drugs like Levodopa.

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    Absorption Rate

    The percentage of orally administered drugs absorbed within a specific time, usually 75% in 1-3 hours.

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    Factors Influencing Absorption

    Elements like gut content (fed vs. fasted) that can affect how well a drug is absorbed.

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    AUC (Area Under the Curve)

    A measure of total drug exposure in the body after administration.

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    Bioavailability (F)

    The fraction of an administered dose of drug that reaches systemic circulation.

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    Factors affecting Bioavailability

    Includes enzyme activity, gastric pH, and intestinal motility.

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    Peak Plasma Concentration

    The highest concentration of drug in the plasma after administration.

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    Sublingual administration

    Delivery of drugs under the tongue for rapid systemic absorption.

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    Buccal administration

    Delivery of drugs between the gum and cheek for systemic effects.

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    GI Motility

    The movement of the digestive tract that affects absorption of drugs.

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    Rectal administration

    Drug delivery via the rectum, bypassing some metabolism.

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    Local vs. Systemic Effects

    Local effects target a specific site, while systemic effects affect the whole body.

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    Splanchnic Blood Flow

    Blood flow to the organs in the digestive system, influencing drug absorption.

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    T max and C max

    T max is the time to reach peak concentration; C max is the peak concentration of a drug in the bloodstream.

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    Gastric Stasis

    A condition where gastric motility is slowed, impacting drug absorption.

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    Modified-Release Preparations

    Drug formulations designed to release medication slowly over time.

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    Absorption Factors

    Elements influencing how well a drug is taken up in the body, like motility and formulation.

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    First-pass Metabolism

    The process where the concentration of a drug is significantly reduced before it reaches systemic circulation.

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    Beclomethasone

    A corticosteroid used to reduce inflammation in the lungs.

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    Bronchodilators

    Medications that relax muscles of the airways, increasing airflow.

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    Hyaluronidase

    An enzyme that increases absorption of drugs by breaking down tissue barriers.

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    Factors affecting absorption

    Elements that impact how quickly and efficiently medication enters the bloodstream.

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    Prolonged Absorption

    The process where drug formulations are designed to extend their duration of action in the body.

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    Adrenaline in Anaesthetics

    Adrenaline is added to local anaesthetics to reduce absorption and prolong their numbing effect.

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    Long-Acting Insulin

    Insulin formulations like glargine and detemir designed for once daily dosing to maintain basal insulin levels.

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    Intrathecal Administration

    A method of delivering drugs into the sub-arachnoid space using a lumbar puncture for specific conditions.

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    Subcutaneous Implantation

    A drug delivery method where solid pellets are placed under the skin for slow continuous absorption.

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    Nusinersen

    An antisense oligonucleotide for spinal muscular atrophy, administered intrathecally.

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    Ranibizumab

    A monoclonal antibody fragment targeting VEGF, used for eye conditions.

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    Aflibercept

    A fusion protein that binds to VEGF, treating wet AMD and other ocular issues.

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    Intravitreal Injection

    Method of delivering medications directly into the eye's vitreous humor.

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    Intravitreal Implants

    Devices releasing corticosteroids slowly for conditions like macular edema.

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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.

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