CLINICAL PHARMACOLOGY

DRUG PRESCRIPTION DIKLAT RUANG TBMM NURUL QOLBI

FRIDA NEILA RAHMATIKANIA. 0811010303

FARMAKOKINETIK

FARMAKODINAMIK

DRUGS

Drug Therapy Decision

Drug designed into a dosage from that can be given to a

patient

D Drug acts to produces its effect on the body

Is the effect on the body beneficial or harmful to the patient?

PharmacologyPharmaceutics

Pharmacokinetics Pharmacodynamics

Therapeutics

A EM

SystemicEnteral

© Oral© Mucous :Sublingual, buccal, nasal, vaginal, rectal

Parenteral © Injection : Intravenous(i.v), intramuscular(i.m), subcutaneous

(s.c), intraperitoneal (i.p), intra-arterial, intrathecalTopikal

©dermal, vaginal, rectal©inhalation

ROUTES OF ADMINISTRATION

The main routes of drug administration and elimination

HOW DO DRUGS WORK?

a. Act on receptors (more)b. Act on ion channel : Ca antagonists, local

anaesthetics, cardiac glycosides, c. Alter enzyme function : COX inhibitors, MAO

inhibitors, AChE inhibitorsd. Act on transporter system : Selective Serotonin

Reuptake Inhibitors, Inhibitors of Na-2Cl-K Symporter (Loop Diuretics)

e. Act on signal transduction protein: Tyrosine Kinase Inhibitors, Type 5 Phosphodiesterase Inhibitors

f. Unconventional mechanism of action

HOW DO DRUGS WORK BY UNCONVENTIONAL MECHANISMS OF ACTION?

• Disrupting of Structural Proteins e.g. vinca alkaloids for cancer, colchicine for gout

• Being Enzymese.g. streptokinase for thrombolysis

• Covalently Linking to Macromoleculese.g. cyclophosphamide for cancer

• Reacting Chemically with Small Moleculese.g. antacids

• Binding Free Molecules or Atomse.g. drugs for heavy metal poisoning, infliximab (anti-TNF)

HOW DO DRUGS WORK BY UNCONVENTIONAL MECHANISMS OF ACTION ? (cont’nd..)

• Being Nutrientse.g. vitamins, minerals

• Exerting Actions Due to Physical Propertiese.g. mannitol (osmotic diuretic), laxatives

• Working Via an Antisense Actione.g. fomivirsen for CMV retininitis in AIDS

• Being Antigens e.g. vaccines

• Having Unknown Mechanisms of Actione.g. general anesthetics

GIT DRUGS

Menghambat prod HCl

AH2• Cimetidine• Ranitidine• Famotidine• Nizatidine

ULCUS PEPTICUM

PPI• Omeprazol

e• Lansoprazole

Melindungi Mukosa

Sucralfate PG Analog• misoprost

ol

Antasida• Mg(OH)2• Al(OH)3

ANTIKONSTIPASI

Laxative

Chathartic

Bulk forming• Psyllium• Polycarbophil• Methylcellulos

e• Mak berserat

Surfactants• Docusate

salts

Stimulants/ Irritant• Bisacodyl• Anthraquinone• Danthron• Sodium

picosulfat

Osmotics• Mg(OH2)• Lactulose

ANTIDIAREOpiate-like Antidiarrheal Agent• Paregoric/ opium

tincture• Diphenoxylate• Difenoxin• Loperamide• codeine

Stool Modifiers• Kaolin• Wheat brand

Antiemetic5HT3 Antagonist• Ondansetron• Granisetron

DA Antagonist

Phenothiazines• Prochlorperazine• Promethazine

Butyrophenones• Haloperidol• droperidolMetoclopramide

Antikolinergik Cannabinoids

Tetrahydrocannabinol• Dronabinol• Nabilone

RESPIRATORY

DRUGS

bronkodilator

Early response :Bronchoconstriction

antiinflamasi

Late response :Inflamation

Hyperreactivity

TERAPI ASMAAg (polutan, alergen)

hindariAg

Ag-Ab/IgE di mast cellantiinflamasi, kromolin

MEDIATOR

Symptom

OBAT ASMA1. Bronkodilator

Β2 antagonis/Simpatomimetik/ adrenergik

Antagonis muskarinik/ M3/Antikolinergik Methylxantin

• Metaproterenol (pot >>)• Formoterol (durasi >>)• Salmeterol/ Salbutamol• Terbutaline• Adrenalin/ Epinephrine• Ephedrine

• Ipratropium bromide• Tiotropium bromide• Atropine

• Theophylline• Teobromine• Caffeine

OBAT ASMA CONT’ND...2. Antiinflamasi

Glukokortikoid Inhibitor degranulasi sel mast

Oral:• Prednisone• Betamethasone (pot, dur

>>)

• Sodium cromolyn (inh) Anti IgE:• Omalizumab

Inhalasi:• Triamcinolone• Budesonide• Fluticasone• Beclomethasone• flunisolide

OBAT ASMA CONT’ND...3. Menghambat Kerja Mediator yg Dilepaskan sel

Mast

Inhibitor Leukotrien AH1

Antagonis R/ Leukotrien (LT-1)• Zafirlukast• Montelukast

Inhibitor Lipoxygenase• Zileuton

OBAT PILEK (DEKONGESTAN)

Sistemik/ Oral Lokal/ NasalSpray: dewasaDrops: < 6 th

• Pseudoephedrine• PPA• Phenylephrine • Ephedrine 0,25%

• Naphazoline HCl 0,05%• Oxymetazoline 0,025. 0,05%• Phenylephrine• Xylometazoline HCl 0,025. 0,1%

MK: agonis R/ α – vasokonstriksi – mukosa & sekresi - hidung longgar

AH1 Gen 2• Cetirizine• Loratadin

e• Terfenadin• Astemizol

Gen 1• Diphenhydrami

ne• Chlorphenirami

ne• Promethazine• Cyproheptadin

e• Clemastine• Bisulepin• Dimetinden• Azatadin• Embramin

MK: prod sekret

OBAT BATUK

perifer central

• Uap menthol, miny. Eucaliptus

• Anestesi lokal topikal (benzocaine, lidocaine)

• Benzonatate

Opioid• Codeine• Morphine• Hydrocodon

e

MK: menekan refleks batuk

1. Antitusif

Non Opioid• DMP

(Dextromethorphan)

OBAT BATUK CONT’ND

• Guaifenesin (GG)• Menthol & Camphor• Ammonium Chloride• Ipecac• Potassium Iodide

MK: mengencerkan sekret – merangsang pengeluaran sekret

2. Ekspektoran

• N-Acetylcysteine MK: menurunkan viskositas sekret dgn merusak ik. Disulfida• DNA-ase (Pulmozyme) MK: merusak DNA mukus scr enzimatik

3. Mukolitik

OBAT ANTINYERI,

ANTI-INFLAMASI,

ANTIPIRETIK

SARAF SENSORISTransmisi

MEKANISME NYERI STIMULUS

KERUSAKAN JARINGAN

MEDIATOR NYERI(HISTAMIN,PG,BRADIKININ,LEOKOTRIEN,SEROTONIN DLL)

RESEPTOR NYERI ( (nociceptor)

MEDULA SPINAL

THALAMUS / KORTEKS PUSAT NYERI

analgesik non narkotik

NSAIDAntiinflamasi

steroid

Transduksi

Modulasi

Persepsi

anestesi lokal

Analgesik narkotik

Anestesi umum

Tx overdosis opioid

Non OpioidAcetaminophen COX-1

Inhibitor

COX-2 Inhibitor• Celecoxib• Rofecoxib• Valdecoxib

Tramadol

OBATANESTESI LOKAL

OBAT

Prokain, tetracaine, cocaineLidokainMepivacainePrilokainBupivakainRopivakain (Naropin)

%

2-4%1-2%1-2%1-2%0,5%

2,5-7,5%

DURASI

1½ jam1-2 jam1-2 jam1-2 jam5-7 jam6-8 jam

MAX

1000 mg500 mg500 mg500mg200 mg

(Levobupivakain) Chirokain

ester

amida

last

<2 hours

<4 hours

4-6 hours

6 to 72 hours

severity

mild MigraineHeadache

Moderate MigraineHeadache

Severe MigraineHeadache

Severe Refractory

over 72 hoursMigraine Headachestatus migrainosus

Obat MigraineTTT

analgesics (Aspirin,Acetaminophen , NSAIDS ) ,

Antiemeticrefractory to above

give Antiemetic , analgesics ,Triptan agents .

refractory to abovegive Other Antiemetic ,

Serotonin Agonist(Dihydroergotamine , Triptans)

refractory to aboveEmergency ttt

5HT 1D agonist

Partial agonist α & 5HT

ANTI-GOUT

ANTIHIPERTENSI

JNC 7:New Blood Pressure Classification

Blood Pressure ClassificationSBP* DBP*(mm Hg)Normal

<120 and <80Prehypertension120-139 or 80-89

Stage 1 hypertension140-159 or 90-99

Stage 2 hypertension160 or 100

Bagaimana Terapi Hipertensi ?

Terapi Non farmakologis : Life style modification

stop merokokdiet : kurangi makanan berlemak & asupan garam,tambah suplemen ion K, Ca, Mg

menurunkan BB aktivitas fisik / OR relaksasi (kurangi stress)

Terapi Farmakologis : Obat antihipertensi

Penggolongan antiHTCCB Nifedipine, verapamil, diltiazem

Vasodilator Oral

Parenteral

Melepaskan NO: hydralazine

Membuka kanal K+: minoxidil

Melepaskan NO: nitroprusside

Membuka kanal K+: diazoxide

ACEI Captopril, enalapril, quinapril, ramipril

Diuretik Thiazid: HCT (hydrochlorothiazide) chlorthalidone

Loop Diuretik: furosemide, torsemide, bumetanide

DHK+: amiloride, triamterene, spironolactone

ARB Irbesartan, losartan, valsartan

Simpatolitik agents

CNS Aktivasi reseptor α2: clonidine, guanabenz, guanfacine

Membentuk neurotransmiter palsu: methyldopa

Ganglion otonom Blok R/ Nikotinik: hexamethonium

Ujung saraf

Menghambat transpor NE ke vesikel sinaps: reserpine

Mengosongkan & memblok pelepasan NE dari tmp penyimpanannya: guanethidine

R/ Adrenergik α1 blocker: prazosin, oxazosin, terazosin

β1 blocker: atenolol, metoprolol

β blocker: propranolol

ANTIDIABETIK

PRINSIP PENATALAKSANAAN DM• Pengaturan diet

– Minum air banyak, susu skim dan minuman berkalorirendah lainnya pada waktu makan

– Hindari makanan manis, gorengan, biskuit, cake– Makanlah dengan waktu yang teratur– Tingkatkan asupan sayuran dua kali tiap makan– Jadikan nasi, roti, kentang, atau sereal sebagai menu utama– Minum air atau minuman bebas gula setiap anda haus

• Latihan jasmaniKegiatan jasmani sehari – hari dan latihan jasmani teratur, 3 –4 x/mgg, selama ± 30 menit : jalan, bersepeda santai, jogging,berenang. Latihan jasmani me BB dan memperbaikisensitifitas thd insulin, serta me uptake glukosa oleh otot(tanpa perlu bantuan insulin)

• Farmakoterapi

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Oral Antidiabetics

Ada 5 kelompok :A. SulfonylureasB. MeglitinideC. BiguanidD. GlitazoneE. Alpha-glucosidase inhibitor

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Mekanisme kerjaOral Antidiabetics (OAD)

• Me absorbsi glukosa : acarbose, biguanid• Me sekresi insulin (secretagogues) :

sulfonilurea 1st, 2nd ,3rd , meglitinide• Me produksi glukosa hepar : biguanid• Me uptake glukosa di perifer :

sulfonilurea 2nd, 3rd , biguanid, thiazolidindion

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ANTIBIOTIK

ANTIBAKTERIMenghambat sintesis dinding sel

Merusak membran plasma

Menghambat sintesis protein

• β laktam• Bacitracin (polipeptid siklik)• Glikopeptid: vancomycin, teicoplanin• Fosfomycin

• Polipeptida: tirosidin, gramisidin, polymyxin, bacitracin

• Polien: nystatin, amphotericin B

Menghambat sintesis as nukleat(Penghambat Girase/ Kuinolon)

• Aminoglikosida: 30S, 50S• Tetrasiklin: tetracycline, oxytetracycline,

chlortetracycline, rolitetracycline, demeclocycline, doxycycline, minocycline

• Linkosamid: clindamycin, lincomycin• Makrolid: erythromycin, josamycin,

spiramycin, roxithromycin, Clarithromycin

Menghambat sintesis metabolit esensial

• Sulfonamid: sulfacarbamid, sulfamethoxazole, sulfalen, sulfasalazine

• Diaminobenzilpirimidin: trimethoprim, tetroxoprim, pyrimethamine

β laktam

Penisilin

• Penisilin G (Benzilpenicillin Na/K)• Penisilin depot: benzilpenicillin-procain,

benzilpenicillin-benzatin• Penisilin oral: penicillin V (phenoxymetylpenicillin),

propycillin• Penisilin oral stabil thp B-laktamase: oxacillin,

dicloxacillin, flucoxacillin• Penisilin spektrum luas: ampicillin, amoxicillin,

bacampicillin (ester sikarboniloksietil)• Penisilin spek luas thp kuman gram (-) yg sulit

dibasmi: mezlocillin, piperacillin)• Inhibitor B-laktamase: clavulenic acid, sulbactam,

tazobactam

Sefalosporin

Karbapenem

Generasi 1: cefadroxil, cefazolin, cefalotin, cefapirin, cefradin (Gr +)

Generasi 2: cefamandole, cefumaxime, cefuroksime, cefotiam (Gr -)

Generasi 3: cefotaxime, ceftriaxone (Gr -)Generasi 4: cefepime (Gr +)

Imipenem, meropenem

Monobaktam Aztreonam

• Generasi 1 (sal kemih): nalidicid acid, pipemidat acid, norfloxacin• Generasi 2 (spek lebar): ofloxacin, ciprofloxacin• Generasi 3 (gram + & atipikal): levofloxacin, grepafloxacin, sparfloxacin• Generasi 4 (gram +, atipikal, anaerob): trovafloxacin, moxyfloxacin, clinafloxacin

Menghambat sintesis as nukleat(Penghambat Girase/ Kuinolon)

• 30S: streptomycin, neomycin, gentaycin, kanamycin, amikacin, sisomycin, tobramycin, spectinomycin

• 50S: (chloramphenicol, azidamphenicol, tiamphenicol), fusidic acid

Aminoglikosida

ANTIMIKOTIK/ ANTIFUNGALMembrane disrupting agents

Ergosterol syn inh

Nucleic acid inh

Amphotericin B, Nystatin

• Imidazol: clotrimazole, miconazole, ketoconazole• Triazol: fluconazole, itraconazole• Alilamin: naftifine• Tiokarbamat: tolnaftate• Morfolin: amorolphylline

Flucytosine

Antimitotic (spindle disruption) Griseofulvin

AntiamoebaNitroimidazol Metronidazole, tinidazole

AntiviralAntiherpes Acyclovir, valacyclovir, brivudine, famcyclovir,

idoxuridine, gancyclovir, foscarnet, cidofovir

Antifungal

Antiviral

Tablet Fe

dr. XXXXXXXX S . P : 02.01.6.1.I.034x S I P : 42x/MLG/DU/V/2002

Alamat Rumah : Jl. Melati no. X MalangPraktek : Jl. Rasuna Said 1 Malang . Telp : 348110Jam : 17.00 – 19.00

Malang, 12 – 11 – 2007

R/ Methampyron ........................ 500 mg. Diazepam ............................... 2 mg. Coffein ................................... 20 mg. Vit B1 ..................................... 50 mg.

Mf . la pulv . da in caps dtd . No . XII.S 1 dd caps . I

P . P Pro : Tn. Dody BB : Alamat : ………… Umur :

50

Inscriptio

Prescriptio

Subscriptio

Signatura

Obat Luar

PULVERES

A