FARMAKOLOGI

BEBAN STUDI = 3 SKS Kuliah = 2 SKS dan Praktikum = 1 SKS Dosen Pengasuh : 5 Orang GBPP SAP yang telah disepakati terdiri dari : 1. Farmakologi Umum (4 jam) 2. Obat ANS & Relaksasi otot (6 jam) 3. Obat Anestesi lokal & umum (4 jam) 4. Obat Diuretik (2 jam) 5. Obat Sedatif-Hipnotik & CNS Stimulan (2 jam) 6. Obat Analgesik, antipiretik & antiinflamasi (2 jam) 7. Obat Hemostatika (2 jam) 8. Hormon & Uterotonika (2 jam) 9. Histamin dan Antihistamin (2 jam)

Pembobotan Penilaian Mata Kuliah :

1. Tugas : bobot 1,5 = 13,64% 2. Kuis/tentamen dll : bobot 1,5 = 13,64% 3. Soft skill : bobot 1 = 9,09% 4. UTS : bobot 2 = 18,8% 5. UAS : bobot 3 = 27,27% 6. Praktikum : bobot 2 = 18.18% bobot 11 = 100%

Presensi : Wajib kuliah :

Nilai E minimal 75% Nilai D,C & BC minimal 50%

PRAKTIKUM (1 SKS)
GBPP SAP disepakati 6 materi praktikum : 1. Cara pemberian obat 2. Obat yg berpengaruh thd. Tekanan darah 3. Mengenal stadium anestesi umum 4. Obat yg berpengaruh pada Diuresis 5. Obat menurunkan rasa nyeri 6. Obat penghambat inflamasi.
Presensi : Wajib Praktikum 100% Kelompok Praktikum Dibagi 6 kelompok : A1 dari kelas A nomor urut 1-45 A2 dari kelas A nomor urut 46-69 B1 dari kelas B nomor urut 1-55 B2 dari kelas B nomor urut 56-70 C dari kelas C ; dan D dari kelas D

BY : D.K. Meles

PHARMACOLOGY
PHARMACON = Drug/ Poison LOGOS = Science PHARMACOLOGY : Science to Study of drug DRUG : All of substance to influence life system application to prevent, diagnostic and therapeutics SCOPE OF PHARMACOLOGY - PHARMACOKINETIC PHARMACODYNAMIC PHARMACOTHERAPEUTIC PHARMACOGNOSI TOXICOLOGY

DRUG All of Substance to influence life process in use to prevent, therapeutics and diagnostic of disease. Have criterion : 1. Effectiveness & Rivesible effect 2. Savety (Margin of savety) Therapeutics Index. 3. High Selectivity

PHARMACOKINETIC

ABSORPTION DISTRIBUTION BIOTRANSFORMATION EXCRETION

ABSORPSI OBAT : Moving Process or to

remove of drug from tissue to another tissue to cross the membrane with spesific mechanism. TRANSPORT PASIVE Different Concentration, No need Energy, non spesific
DIFFUSION NON-IONIC FILTRATION POROUS FASCILITATIVE DIFFUSION CARRIER

1.

2.

TRANSPORT ACTIVE OPPOSITION GRADIENS CONCENTRATION, Need Energy & Spesificity

PINOSITOSIS/ EXOSITOSIS/ ENDOSITOSIS.

3.

DRUG ABSORBTION Account in % from drug dose DRUG BIOAVAILABILITY Prosentage drug to reach site of action. Was count from dose of drug (for drug sistemik only). FACTOR2 TO INFLUENCE RATE OF DRUG ABSORBTION : 1. Route of drug application 2. Circulation of place application drug. 3. Solubelity of drug 4. Ionization Rate of Drug 5. Broad of absorbtion area. 6. Size of molecule particle of drug 7. Drug Formulation

ROUTE OF DRUG ADMINISTRATION

1. 2. 3. 4. ENTERAL (SUBLINGUAL, PER-ORAL, PER-ANAL) PARENTERAL (SC., IM., IV., INTRAPERITONEAL) TOPICAL (SKIN, MUCOSA) PERINHALATION.

Sub-Lingual :
Condition : Iritation, Damage by gastric Acid &Damage from drug metabolis.To clause Dilute in saliva, Non-iritan & Lipofilik.

PER-ORAL :

General, easy, safety and cheap. Influenced by GIT motility Absorbtion Diffusi pasive, depend on rate of disolution & disintegration. No application in consciousless.

PER-RECTUM Applicated in condition : gastric iritation, vomiting, damage by gastric acid.

Rate of absorbtion irreguler, Sometimes rectum irritation

Per-injection :
Benefid : Quick in absorbtion, vomit condition consciousless and emergency applicated Wickedness : must be sterilzation, cant self uses, pain, & ralative more expensive.

Intra-Vena :

No absorbtion process direct in blood Onset dan Duration quickly Iritatif drug can applicated Drug toxicity Low in therapeutics Index Must be carefully

Intra-muskuler (I.M.) dan Sub-kutan (S.C.) Condition : non-iritan drug, water soluble or suspention form. Quick in effect (im=Sc).

Intraperitoneal : In animal experimental applicated only opten infection. Subtitute i.v. route Per-inhalation : Use in gas form drug. Absorbtion a cross epithel mucosa & quick. Need tools/ specific methode Dificult in dose count
Topical Unguentum, drops for mocosa & skin

DRUG DISTRBUTION
AFTER ABSORBTION Extracelluler Fluids (Plasma + 4%,Interstesiil + 13%). DRUG Protein plasma bound, Inactivation/ metabolism process, Bound in reseptor Respon/ drug effect, Exretion Renal Intraseluler Fluid + 41% DRUG Reseptor drug respons Prot. tissue. Non Spesific & Reversibel. Bound in Fat Drug Reservoir. Metabolism (Biotransformation). Drugs lipid soluble easy a cross membrane and distribution to intracelluler fluids, distribusi ke intraseluler. Opposite on non lipid soluble drug

BIOTRANSFORMATION:
MECHANISME TO CHANGE DRUGS STRUCTURE TO BE : * Decrease in fat solublelity * to break in ionized * Decrease in protein plasm/ tissue bound. Biotransformation Drug to be in active Metabolite Aktive : Prontosil (In vitro) Sulfanilamid. Proguanil Metabilite aktif.

MECHANISME OF BIOTRANSFORMATION
DRUG ABSORBTION DISTRIBUSTION protein bound reseptor bound Excretion BIOTRANSFORMATION (metabolism) FASE I FASE II

1. 2. 3. 4.

Oksidation cytochrom axidase Reduction Declorinasi HidrolysisEsterase, Amidase Hydrasi Hidrolase

BM < 300 BM> 300

1. Sulfation Sulfonyl transferase 2. Glucorhonidation G.transferase 3. Conjugation As.Glukoronat 4. AcetYlation, Methylation

BM< 300

URINE Filtration, Secretion

PHARMAKODYNAMIC
Pupose : To know drug effect To know drug Interaction To know spectrum drug respons

MECHANISM OF ACTION : 1. Interaction with drug reseptor to change biochemical & Physiological process ( Neurotransmitter) Respons. 2. Physical-chemist Characteristic of drug Drug respons 3. Chelating Agent drug respons 4. Drug incorporation with celluler structure drug respon

DRUGS INTERACTION

SYNERGISM ADITIVE & POTENTIATIVE ANTAGONISM : * A. Chemist : Heparin X Protamin * A. Functional/Physiological ( NE X Histamin) * A. Selective Receptor Drugs. A. Selective Competitive : In seem receptor. Riversible : ACH x Atropin Irreversible : NE x Prazosin A. Selective non-competitive Different receptor, D-R bound cant break in highly dose. Papaverin x Histamin ( Papaverin x ACH)

DOSE :

measure / quantity of drug to give for individual until a cross activity threshold but cant cross Toxicity threshold. Margin Of safety = LD50 : ED50
INFLUANCE FACTOR OF DOSE : 1. BODY WEIGHT( BW) 2. OLD 3. RUST 4. SeX 5. Time of administration 6. Patological Disholder 7. Genetic factor 8. Tolerance

DRUG TOXICITY

Wrong in drug administration : Tetracycline (I.V) konvulsive. Penicilline (I.V.) Presipitation. To remain the drug effect ( Excessive dose/ Over dose, Ren & liver malfunction, genetic factor, drug interaction).

Hypersensitive reaction (Allergy) : Dermatitis, Asthma, Shyok anafilactic, damage in liver & ren, damage in bonemarrow.
Blood discrasia, as well as Leucopenia, aplastic anaemia, haemolytic anaemia, thrombositopenia. Toxicity in liver & ren Teratogenic effect.

RESEARCH OF DRUG
1.

TO INVENTION THE NEW DRUG * EMPERICALLY * RASIONALITY * UNEXPECTED (KEBETULAN) * SCREENING PROCESS PREKLINIK TRIAL * Activity Test & Side effect Test * Uji Pharmacokinetic dan Pharmacodynamic * Uji Farmacy yang meliputi : * Uji Kualitative dan Kuantitative bahan * Uji Stability * Uji Sifat Physic dan Chemist * Uji drug formulation * Uji general toxicity : Uji Acute , Sub Acute & Chronic Toxicity Test * Uji specific toxicity : Uji Teratogenic, Mutagenic dan Carcinogenic

2.

3.

KLINICAL TRIAL Devide 4 fase dan Uji Monitoring drug side effect (MESO).