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Physicochemical Properties of Drugs in relation to Drug Action

Physicochemical Properties of Drugs in relation to Drug Action. Roselyn A. Naranjo USPF, College of Pharmacy www.roselynnaranjo.vze.com roselean@gmail.com. DRUG-RECEPTOR INTERACTIONS. ORAL. Systemic Circulation. Intramuscular Subcutaneous Intravenous. DRUG-RECEPTOR INTERACTIONS. ORAL.

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Physicochemical Properties of Drugs in relation to Drug Action

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  1. Physicochemical Properties of Drugs in relation to Drug Action Roselyn A. Naranjo USPF, College of Pharmacy www.roselynnaranjo.vze.com roselean@gmail.com

  2. DRUG-RECEPTOR INTERACTIONS ORAL Systemic Circulation Intramuscular Subcutaneous Intravenous

  3. DRUG-RECEPTOR INTERACTIONS ORAL Systemic Circulation Intramuscular Subcutaneous Intravenous

  4. DRUG-RECEPTOR INTERACTIONS receptor + = drug good fit • more drug molecules are bounded • Favors irreversible reaction • Desired pharmacologic response

  5. DRUG-RECEPTOR INTERACTIONS + = receptor drug poor fit • Small amount of drug molecules are bounded • Favors reversible reaction • No response • Ineffective drug

  6. DRUG-RECEPTOR INTERACTIONS Variables that affects drug binding - OH – O = \ / C - OH - ll C / \ • Structural class • 3D shape of molecule • Type of chemical bonds

  7. DRUG-RECEPTOR INTERACTIONS Drugs with the same Pharmacologic class & structural features RECEPTOR SITE EFFECT DRUGS • Barbiturates • Depressant effects • Specific CNS receptors • Hydantoin • Anticonvulsant response • Specific CNS receptors • Benzodiazepines • Anxiolytic activity • GABA receptors • Penicillin • Inhibit bacterial cell wall construction • Specific enzymes • Cephalosporins • Inhibit bacterial cell wall construction • Tetracyclines • Bacterial wall ribosomes

  8. DRUG-RECEPTOR INTERACTIONS • RECEPTORS First Receptor Model Enzymes • Acetylcholinesterase • Dihydrofolate reductase • Angiotensin • HIV protease-converting enzymes

  9. H H O \ l ll N – C – C - OH / l H R H DRUG-RECEPTOR INTERACTIONS • RECEPTORS Proteins (+) (-) H - receptors are not distributed equally Acid group Amine group Amine group Alkyl group - behave differently

  10. DRUG-RECEPTOR INTERACTIONS • RECEPTORS Proteins Drug therapy Produce 2 effects • Pharmacologic response • Adverse reactions

  11. DRUG-RECEPTOR INTERACTIONS • RECEPTORS Proteins Example Paste tamoxifen Structure here ANTAGONIST in the Mammary Gland Pharmacologic response Adverse effect • Prolonged treatment results to endometrial cancer due to the response of estrogen uterine receptors • For estrogen-sensitive breast cancer AGONIST in the Uterus & Bone • For reducing bone loss from osteoporosis

  12. DRUG-RECEPTOR INTERACTIONS • RECEPTORS Proteins Example Paste sildenafil Structure here NO EFFECT in Angina Unexpected Results Expected effect • Effective inhibitor of an enzyme found in the corpus cavernosum • Inhibit phosphodiesterase that would treat angina EFFECTIVE in erectile dysfunction • Vasodilate the blood vessels in the male organ that leads to penile erection

  13. DRUG-RECEPTOR INTERACTIONS • FORCES INVOLVED Biological response Biological receptor site Bonding force

  14. DRUG-RECEPTOR INTERACTIONS • FORCES INVOLVED Biological response Ionic bond/weaker • short-acting • reversile Bonding force Covalent bond/stronger • long-lasting effect • irreversible

  15. DRUG-RECEPTOR INTERACTIONS • Types of Chemical Bonds H l R-N-H-O l C - R’ H O (+)---(-) (+)---(-)

  16. DRUG-RECEPTOR INTERACTIONS Types of Chemical Bonds - OH – O = \ / C - OH - ll C / \ l O = C ....:NR3 l δ- δ+

  17. DRUG-RECEPTOR INTERACTIONS • Cis& trans structure formation • FORCES INVOLVED

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