Rebecca Review

Rebecca Review - Routes of Drug Administration Oral Topical...

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Routes of Drug Administration Oral Topical (Percutaneous) Rectal or Vaginal Pulmonal Parenteral Types of Orally Administered Drugs Pills (single dose) Tablets Coated Tablets (shell) Matrix Tablets (carrier meshwork) Capsules (gelatin shell) Troches/Lozenges Solutions Percutaneous Drug Administration Ointment + Lipophilic cream Paste Lotion Gels Can be single or multilayer, or contained in a reservoir Other Topicals Eye Drops Nose Drops Pulmonary Formulations Suppositories Parenteral Drug Administration Ampules Vials Cartridge Ampules Infusions Advantage: 100% Absorption, enters circulation without hepatic elim, better bioavailability of hydrophilic drugs
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Types of Barriers for Drug Distribution/Absorption External Absorption Barriers: (epithelial layer on skin, lung, intestine—Lipophilic barrier) Internal Blood-Tissue Barriers: Cardiac muscle, endocrine glands, gut, liver, CNS Drug Distribution Passive Diffusion Active Transport Receptor-mediated Endocytosis [DRUG] IS A FUNCTION OF ABSORBTION AND ELIMINATION! Bioavailability The AUC of the administered drug divided by the AUC of the intraveneously administered drug IV>TD>IM=SC>Rectal>Oral=Inhal Volume of Distribution Rate of Elimination Vd=Amt of drug in the mody/[drug] R of E: Via kidney (filtration) or liver (metabolism) Usually first order kinetics 3 drugs have zero-order kinetics Clearance Rate of Elim/[Drug] Rate of Elim= k*Cp*Vd K= ln2/T ½ CL= K*Vd
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Phase I Reactions Convert parent compound into more polar metabolite Add/unmask functional group: OH, SH, NH2, COOH, etc Oxidation, Reduction, hydrolytic cleavage, Alkylation, Dealkylation, etc… Phase II Reactions Conjugation with endogenous substrate (increase aq solubility) Conjugation with gucoronide, sulfate, acetate, amino acid MFO Mixed Function Oxidases Require reducing agent and molecular oxygen Two enzymes: 1) Flavoprotein, NADPH-cytochrome c reductase 2) Cytochrome P450 (electron acceptor); CYP P450 Enzymes PPAR ligands, CYP1, CYP2E, CYP2B Polymorphisms cause changes in drug metab: CYP2C19, CYP2B, CYP2D6 Induction of P450 enzymes=metabolize drug Conjugation Reactions Glucoronidation Sulfation Acetylation Amino acid Conj Glutathione Conj Fatty acid Conj Condensation Reaction
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Monoamine Oxidases (MAO) Catalyze oxidative deamination of endogenous catecholamines (epinephrine) Lacated in never terminals and peripheral tissues Many drug/food interactions! (cheese, wine) Inhib by MAO inhib Therapeutic Index Maximum non-toxic dose/Min effective dose Doesn’t take into account variability btw indivs LD50/ED50 Agonist Can be drugs or endogenous ligands for the receptor Increasing [agonist] will produce increase in biological response Full:evokes 100% max possible effect Partial: not 100% Antagonist Block or reverse effect of agonist No effect on their own Competitive, Non-competitive, inverse agonist (triggers neg response) Four major drug targets Receptor Enzyme Ion Channel Transporter
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Ca++ as a Second Messenger Regulates many cellular and phys. Responses
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This note was uploaded on 04/13/2010 for the course BIMM bimm 118 taught by Professor David during the Winter '09 term at UCSD.

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Rebecca Review - Routes of Drug Administration Oral Topical...

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