Depot Injectables Overview
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Questions and Answers

What is the primary purpose of inotuzumab when administered to leukemia patients?

  • To provide an external source of chemotherapy
  • To target the CD22 antigen on leukemia cells (correct)
  • To increase blood circulation in the tumor region
  • To enhance immune response against healthy cells

Which drug delivery method combines drug diffusion with polymer degradation for controlled drug release?

  • Depot injectables
  • Liquid crystal nanotubes
  • Mechanical implants
  • Bioerodible microspheres (correct)

Which of the following systems is NOT typically associated with enhancing drug targeting and minimizing off-target effects?

  • Depot injectables (correct)
  • Antibody-drug conjugates
  • Albumin nanoparticles
  • Liposomes

What characterizes the Atrogel system in drug delivery?

<p>It forms a drug-releasing matrix in situ (B)</p> Signup and view all the answers

Which method of drug delivery provides the longest duration for sustained release?

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

What is the primary characteristic of depot injectables?

<p>They are administered subcutaneously or intramuscularly. (B)</p> Signup and view all the answers

How do prodrugs function within depot injections?

<p>They remain lipophilic and release the active drug slowly. (D)</p> Signup and view all the answers

What makes bioerodible microspheres a more advanced form of depot injectables?

<p>They rely on drug diffusion and polymer breakdown for release. (C)</p> Signup and view all the answers

Which of the following components is present in Lupron Depot?

<p>Glycolic acid and polylactic acid copolymer (D)</p> Signup and view all the answers

What mechanism does the Atrogel delivery system use for extended drug release?

<p>Formation of a drug-containing matrix upon contact with bodily fluids (D)</p> Signup and view all the answers

Which statement about depot injectables is incorrect?

<p>Depot injections are primarily used for rapid drug absorption. (A)</p> Signup and view all the answers

In terms of formulation, what distinguishes Invega Sustenna from other depot injectables?

<p>It utilizes a palmitate ester for sustained release. (C)</p> Signup and view all the answers

Which aspect of depot injection formulations influences the duration of drug release?

<p>The solubility and metabolism of the drug (B)</p> Signup and view all the answers

What is the main purpose of SUBLOCADE?

<p>To manage opioid use disorder (B)</p> Signup and view all the answers

What characterizes the Somatuline Depot delivery system?

<p>It releases medication over 4 weeks through self-assembled nanotubes. (D)</p> Signup and view all the answers

What are the benefits of using an implantable infusion pump for drug delivery?

<p>It provides both spatial and temporal control over drug delivery. (D)</p> Signup and view all the answers

Which of the following implants is specifically designed for localized delivery of a chemotherapy agent?

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

What component of Nexplanon aids in its detection by X-ray?

<p>The barium sulfate content (D)</p> Signup and view all the answers

What is a unique characteristic of bioerodible matrix implants?

<p>They release drugs through polymer degradation and diffusion. (A)</p> Signup and view all the answers

Which type of drug delivery system provides zero-order release requiring surgical insertion?

<p>Membrane-controlled reservoir systems (D)</p> Signup and view all the answers

In which condition is a mechanical implant's infusion pump, like the Entera 3000, primarily used?

<p>Intrahepatic chemotherapy for liver tumors (B)</p> Signup and view all the answers

What is the primary method of drug release for polymer implants?

<p>Diffusion and degradation of the polymer (D)</p> Signup and view all the answers

What aspect of subcutaneous tissue makes it suitable for implantable drug delivery devices?

<p>Low reactivity minimizes discomfort and promotes retention. (B)</p> Signup and view all the answers

What type of drug delivery system exemplifies the use of a solid polyethylene vinyl acetate polymer matrix?

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

What method does the SynchroMed 3 use to propel medication from the reservoir?

<p>Mechanical pumping by rotating cams (A)</p> Signup and view all the answers

Which implant is used for the treatment of central precocious puberty?

<p>Hysterelin Acetate Implant (A)</p> Signup and view all the answers

Which statement accurately describes the characteristics of external pumps?

<p>They deliver medication using positive pressure from outside the body. (D)</p> Signup and view all the answers

What is a primary feature of insulin pumps in modern medicine?

<p>They provide automated insulin delivery based on real-time glucose levels. (A)</p> Signup and view all the answers

What mechanism do elastomeric infusion pumps use to deliver medication?

<p>Elastic membrane contraction. (C)</p> Signup and view all the answers

Which of the following statements accurately describes the function of Patient-Controlled Analgesia (PCA) pumps?

<p>They enable patients to self-administer medication within set limits. (B)</p> Signup and view all the answers

What role do stealth liposomes play in drug delivery?

<p>They prolong circulation time by evading the Mononuclear Phagocyte System. (C)</p> Signup and view all the answers

What is a distinguishing property of albumin nanoparticles as drug carriers?

<p>They improve the tolerability of paclitaxel without toxic excipients. (B)</p> Signup and view all the answers

Which of the following best describes liposomes?

<p>They consist of a lipid bilayer that surrounds an aqueous core. (B)</p> Signup and view all the answers

What is the primary function of particulate drug carriers in spatial control?

<p>To facilitate targeted delivery to specific tissues. (B)</p> Signup and view all the answers

Which type of infusion pump is designed primarily for home infusion therapy?

<p>Ambulatory infusion pumps. (A)</p> Signup and view all the answers

What is a unique characteristic of Abraxane as a drug formulation?

<p>It is a suspension of albumin-bound nanoparticles. (A)</p> Signup and view all the answers

How do antibody-drug conjugates (ADCs) deliver cytotoxic drugs specifically?

<p>By binding to receptors that facilitate endocytosis. (B)</p> Signup and view all the answers

What potential advantage does pegylation confer to liposomal formulations like Doxil?

<p>Enhances the drug's half-life and reduces cardiac toxicity. (B)</p> Signup and view all the answers

Which drug is an example of an antibody-drug conjugate used in cancer therapy?

<p>Inotuzumab ozogamicin. (A)</p> Signup and view all the answers

What limits the accuracy of elastomeric infusion pumps in medication delivery?

<p>The predetermined flow rate set by the pump's design. (A)</p> Signup and view all the answers

What type of rate delivery control do hospital infusion pumps provide?

<p>Continuous and intermittent infusion rates. (B)</p> Signup and view all the answers

Flashcards

Depot Injectables

Long-acting drug delivery method, usually injected subcutaneously or intramuscularly.

Suspensions (Drug Delivery)

Uses slowly dissolving crystals in water or oil to prolong drug release.

Prodrugs

Inactive compounds that the body converts into active drugs.

Lipophilic

Fat-soluble; important for prodrugs remaining in fatty tissue for sustained release.

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Bioerodible Microspheres

Drug particles in a biodegradable polymer. Release by polymer breakdown and drug diffusion.

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Lupron Depot (example)

Bioerodible microsphere containing a hormone agonist for 1-4 month releases.

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Atrigel Delivery System

Drug in a biocompatible solvent forming a matrix that solidifies at the injection site.

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Drug Diffusion

Release mechanism within bioerodible microspheres, where drugs spread through the polymer matrix.

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Stored Energy Disposable Pumps

Pumps that use mechanisms like springs, gas pressure, or elastic rebound to deliver medication.

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Hospital Infusion Pumps

Pumps used in hospitals to deliver medication intravenously.

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Ambulatory Infusion Pumps

Portable pumps used for home infusion therapy or outpatient use.

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PCA Pumps

Pumps that allow patients to self-administer pain medication with safety limits.

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Insulin Pumps

Pumps that deliver insulin based on real-time glucose levels.

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Elastomeric Infusion Pumps

Disposable pumps using an elastic membrane to deliver medication.

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Spatial Control in Drug Delivery

Targeting medication to specific sites within the body.

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Particulate Drug Carriers

Systems like liposomes or nanoparticles that deliver drugs to target cells.

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Liposomes

Spherical vesicles with a phospholipid bilayer, encapsulating drugs.

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Stealth Liposomes

Liposomes coated with PEG to evade macrophage clearance.

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Doxil (pegylated liposomal doxorubicin)

A liposomal formulation of doxorubicin used for Kaposi's sarcoma.

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Albumin Nanoparticles

Albumin-based particles used as drug carriers.

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Abraxane (paclitaxel protein-bound particles)

Paclitaxel bound to albumin nanoparticles for improved delivery.

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Antibody-Drug Conjugates (ADCs)

Drug-antibody combos that target specific cells for delivery.

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Besponsa (inotuzumab ozogamicin)

An ADC for a type of leukemia.

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Atrogel System

A drug delivery system that utilizes a solidified polymer depot to provide sustained release of medication. Buprenorphine, for example, is formulated using Atrogel and provides a 1-month release.

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Liquid Crystal Nanotube

A drug delivery system that uses self-assembled nanotubes containing medication to provide sustained release. Somatuline Depot is an example, releasing lanreotide for 4 weeks.

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Implants

Devices placed subcutaneously for long-term drug delivery, taking advantage of the characteristics of subcutaneous tissue. They can be polymer or mechanical.

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Subcutaneous Tissue Characteristics

The subcutaneous tissue is ideal for implants due to its rich fat content, poor blood perfusion and nerve density, and low reactivity to foreign matter.

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Polymer Implants

Implants made of biodegradable or non-biodegradable polymers that control drug release. There are two main types: membrane-controlled reservoir and bioerodible matrix.

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Membrane-Controlled Reservoir System

A polymer implant where a drug reservoir is surrounded by a rate-controlling membrane, providing predictable and consistent drug release.

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Nexplanon

A contraceptive implant that exemplifies a membrane-controlled reservoir system. It releases contraceptive medication for up to 3 years.

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Bioerodible Matrix Implants

Biodegradable implants where the polymer matrix degrades gradually, releasing the drug through diffusion and erosion.

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Gliadel Wafer

A unique biodegradable intracranial implant that delivers carmustine (chemotherapy) locally, targeting residual cancer cells.

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Mechanical Implants

Implants that utilize pumps to deliver medication under positive pressure. They typically consist of a pump, reservoir, and catheter.

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SynchroMed 3

An implantable infusion system with a peristaltic pumping mechanism, delivering medication at a controlled rate.

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Intrathecal Pump

A mechanical implant used for delivering medication to manage spasticity, with the catheter tip placed in the spinal cord.

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Programmability

The ability to adjust some implantable pumps, like SynchroMed 3, allowing patients to control their pain management within physician-specified limits.

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External Pumps

Devices worn outside the body to deliver medication under positive pressure, similar to implantable pumps.

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Targeted Drug Delivery

Delivering medication precisely to specific locations within the body, enhancing efficacy and minimizing side effects.

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Inotuzumab Ozogamicin (Besponsa)

A specific type of ADC used to treat certain types of leukemia. The antibody targets CD22 on leukemia cells, delivering the drug ozogamicin directly to the cancer.

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Study Notes

Depot Injectables

  • Suspensions: Slow-dissolving drug suspensions (water or oil) are used for extended release. Drugs must dissolve into molecules to be absorbed. Example: 3-month depot injectables.
  • Prodrugs: Inactive "pro-drugs" are metabolized in the body to release the active drug. Lipophilic (fat-soluble) prodrugs dissolve slowly, releasing the active drug over time. Examples: Depo-Testosterone, Invega Sustenna. Invega Sustenna uses a palmitate ester for extended release.
  • Bioerodible Microspheres: Drug particles in a biodegradable polymer matrix. Drug release is via polymer diffusion and breakdown. Example: Lupron Depot (polylactic acid and polyglycolic acid). Available in 1-month, 3-month, and 4-month release durations.

Atrigel Delivery System

  • Mechanism: Dissolving the drug, liquid injection solidifies the drug into a matrix. Example: SUBLOCADE (buprenorphine) - 1-month subcutaneous release of buprenorphine. Biodegradable, breaks down into lactic and glycolic acid.

Liquid Crystal Nanotubes

  • Mechanism: Lanreotide peptide forms nanotubes. Somatuline Depot uses this. Depot forms from nanotubes, releasing medication over 4 weeks (primarily as nanotubes, with a small initial dose from free lanreotide).

Implants

  • Subcutaneous Tissue Characteristics: Rich in fat, poor blood/nerve perfusion, low reactivity to foreign matter.
  • Polymer Implants: Biodegradable or non-biodegradable polymers control drug release.
    • Membrane-Controlled Reservoir Systems: Rate-controlling membrane surrounds a drug reservoir (e.g., Nexplanon, a contraceptive implant, containing contraceptive medication in polyethylene vinyl acetate). Provides up to 3 years of contraception, zero-order release, surgical insertion/removal. Contains barium sulfate for radio-opaqueness.
    • Bioerodible Matrix Implants: Biodegradable, no surgical removal. Drug release by diffusion and polymer degradation. Example: contraceptive implant - 1-month or 3-month drug release, composed of polylactic acid and polyglycolic acid, which are broken down to lactic and glycolic acid by water.
  • Gliadel Wafer: Biodegradable intracranial implant delivering carmustine (a chemotherapeutic agent) to residual tumor cells. High concentration delivered locally, minimizing systemic exposure (1000x higher than intravenous dose). Carmustine dispersed in a biodegradable matrix.

Mechanical Implants: Implantable Infusion Pumps

  • Mechanism: Pumps deliver medication under pressure. Reservoir, pump, catheter surgically implanted.
  • Examples:
    • SynchroMed 3: Peristaltic pumping mechanism, refillable reservoir.
    • Intrathecal pump for spasticity: For medication delivery to the spinal cord.
    • Intrahepatic artery infusion pump (Entera 3000): for targeted liver chemotherapy.
  • Programmability: Some pumps (e.g., SynchroMed 3) can be programmed by a physician for personalized pain management (patient-controlled analgesia or PCA).

External Pumps

  • Mechanism: Deliver medication using positive pressure.
    • Stored energy disposable pumps: Use a spring-loaded, gas pressure or elastic mechanism.
    • Hospital infusion pumps: Precise rate control, various delivery modes (continuous, intermittent, bolus).
    • Ambulatory infusion pumps: Smaller, portable, for home use.
    • PCA pumps: Patient controlled pain medication delivery (within predefined parameters).
    • Insulin pumps: Modern ones often integrate with CGM (continuous glucose monitors) for automated insulin delivery. Example: Dexcom G7 CGM system, MiniMed 780g system.
    • Elastomeric infusion pumps: Utilise an elastic membrane (balloon), filled with drug fluid. Contraction forces drug fluid through catheter, controlled by flow restrictor; often simpler and portable but less accurate than electronic pumps.

Spatial Control and Targeted Drug Delivery

  • Particulate Drug Carriers: Liposomes, albumin nanoparticles, antibodies deliver targeted doses.
  • Liposomes: Spherical vesicles containing hydrophilic or lipophilic drugs. Stealth liposomes prevent immediate recognition by macrophages. Example: Doxil (pegylated liposomal doxorubicin), DaunoXome (liposomal daunorubicin), Vyxeos (liposomal daunorubicin and cytarabine), Ambisome (liposomal amphotericin B).
  • Albumin Nanoparticles: Example Abraxane (paclitaxel protein-bound particles): using albumin to carry paclitaxel, avoiding toxic excipients. Suspension form administered intravenously in tiny nanoparticles.
  • Antibody-Drug Conjugates (ADCs): Example: Besponsa (inotuzumab ozogamicin). Antibody targets leukemia cells, delivers cytotoxic drug into the cancer cell.

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This quiz covers the key concepts related to depot injectables, including suspensions, prodrugs, and bioerodible microspheres. It highlights examples such as Invega Sustenna and Lupron Depot along with their mechanisms of action and release durations.

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