ADME, Prodrugs, and Excretion - lect 16

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Prodrug

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Inactive compound converted into an active drug within the body through metabolic processes.

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Enalapril

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Inactive form of enalapril, converted to enalaprilat in the body to improve oral bioavailability.

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Flashcards covering key vocabulary and concepts from the lecture notes.

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26 Terms

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Prodrug

Inactive compound converted into an active drug within the body through metabolic processes.

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Enalapril

Inactive form of enalapril, converted to enalaprilat in the body to improve oral bioavailability.

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Enalaprilat

Active drug converted from enalapril within the body.

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Controlled Release

The ability to release a drug slowly over time, maintaining a therapeutic window without frequent dosing.

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Azathioprine

Prodrug converted to mercaptopurine under ophthalmic conditions for controlled release.

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Mercaptopurine

Immunosuppressant drug released from azathioprine.

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Cyclophosphamide

Prodrug of phosphoramide mustard that masks toxicity until activated at the point of action.

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Chloramphenicol

An antibiotic with poor solubility and taste, improved via prodrug forms like chloramphenicol sodium succinate.

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Methanamine

Prodrug used to treat urinary tract infections by converting to formaldehyde in acidic conditions.

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Fluorouracil

Inhibits DNA synthesis by acting as a false substrate to stop cancer cells from replicating.

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Elimination

Drugs are converted into metabolites, removed through urine, or mixed with the bile and feces.

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Nephrons

Functional unit of the kidney involved in filtering water and waste products from the blood to form urine.

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Passive Process

The process by which the body retains water while removing waste products.

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Active Process

The process by which the body retains some sugars, amino acids, or other molecules.

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Solubility

The extent to which a compound dissolves in a solvent, crucial for drug absorption and excretion.

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Polymorphism

Different crystal forms of a compound, affecting properties like melting point and solubility.

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Therapeutic Dose

The dose of a drug needed to achieve the desired therapeutic effect.

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Tweaking Acidity

Add electron withdrawing groups to increase acidity or electron pushing groups to make it more basic.

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Cyclodextrin

A ring of glucose molecules that has a slightly favored pocket, which can take in some kind of hydrophobic.

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Vesicles

Synthetic phospholipids used to encapsulate and deliver drugs.

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Bulkers or Fillers

Material added to a drug formulation to increase its bulk, improve taste, or aid processing.

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Coating Agent

Coating agent to make the improve the taste

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Lubricant

Added to a drug formulation to make it run smoothly through manufacturing equipment.

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Preservatives

Added to a drug product to prevent microbial contamination and degradation.

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Phase one

Metabolic reactions that introduce or expose polar functional groups on a drug molecule.

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Phase two

Reactions that conjugate a drug molecule with a polar molecule, increasing its water solubility.