Clinical Pharmacology TBMM Frida

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CLINICAL

PHARMACOLOGY
DRUG PRESCRIPTION
DIKLAT RUANG TBMM NURUL QOLBI
FRIDA NEILA RAHMATIKA
NIA. 0811010303

DRUGS

FARMAKOKINETI
K

FARMAKODINAMI
K

Drug Therapy Decision

Drug designed into a


dosage from that
can be given to a
patient

Drug acts to produces


its effect on the
body

Pharmacokinetics
Pharmaceutics

Pharmacodynamics

Pharmacology

Is the effect on the


body beneficial
or harmful to
the patient?

Therapeutics

ROUTES OF ADMINISTRATION
Systemic
Enteral
Oral
Mucous :Sublingual, buccal, nasal, vaginal, rectal

Parenteral
Injection : Intravenous(i.v), intramuscular(i.m), subcutaneous
(s.c), intraperitoneal (i.p), intra-arterial, intrathecal

Topikal
dermal, vaginal, rectal
inhalation

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 inhibitors
d. 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 Enzymes
e.g. streptokinase for thrombolysis

Covalently Linking to Macromolecules


e.g. cyclophosphamide for cancer
Reacting Chemically with Small Molecules
e.g. antacids

Binding Free Molecules or Atoms


e.g. drugs for heavy metal poisoning, infliximab (anti-TNF)

HOW DO DRUGS WORK BY UNCONVENTIONAL


MECHANISMS OF ACTION ? (contnd..)

Being Nutrients
e.g. vitamins, minerals

Exerting Actions Due to Physical Properties


e.g. mannitol (osmotic diuretic), laxatives
Working Via an Antisense Action
e.g. fomivirsen for CMV retininitis in AIDS

Being Antigens
e.g. vaccines

Having Unknown Mechanisms of Action


e.g. general anesthetics

GIT DRUGS

ULCUS PEPTICUM

Menghambat prod HCl

AH2
Cimetidine
Ranitidine
Famotidine
Nizatidine

PPI
Omeprazol
e
Lansoprazole

Melindungi Mukosa

Sucralfate

PG Analog
misoprost
ol

Antasida
Mg(OH)2
Al(OH)3

ANTIKONSTIPASI

Laxative

Bulk forming
Psyllium
Polycarbophil
Methylcellulos
e
Mak berserat

Surfactants
Docusate
salts

Stimulants/
Irritant
Bisacodyl
Anthraquinone
Danthron
Sodium
picosulfat

Chathartic

Osmotics
Mg(OH2)
Lactulose

ANTIDIARE
Opiate-like Antidiarrheal
Agent
Paregoric/ opium
tincture
Diphenoxylate
Difenoxin
Loperamide
codeine

Stool Modifiers
Kaolin
Wheat brand

Antiemetic
5HT3
Antagonist
Ondansetron
Granisetron

DA Antagonist
Phenothiazines
Prochlorperazine
Promethazine
Butyrophenones
Haloperidol
droperidol
Metoclopramide

Antikolinergik

Cannabinoids
Tetrahydrocannabi
nol
Dronabinol
Nabilone

RESPIRATORY
DRUGS

TERAPI ASMA
Ag (polutan, alergen)
hindariAg

Ag-Ab/IgE di mast cell


bronkodilator

antiinflamasi, kromolin
antiinflamasi

MEDIATOR

Early response :
Bronchoconstriction
Symptom

Late response :
Inflamation
Hyperreactivity

OBAT ASMA

1. Bronkodilator
2 antagonis/
Simpatomimetik/ adrenergik

Metaproterenol (pot >>)


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

Antagonis muskarinik/ M3/


Antikolinergik
Ipratropium bromide
Tiotropium bromide
Atropine

Methylxantin
Theophylline
Teobromine
Caffeine

OBAT ASMA CONTND...

2. Antiinflamasi
Glukokortikoid

Oral:
Prednisone
Betamethasone (pot, dur
>>)
Inhalasi:
Triamcinolone
Budesonide
Fluticasone
Beclomethasone
flunisolide

Inhibitor degranulasi sel mast

Sodium cromolyn (inh)

Anti IgE:
Omalizumab

OBAT ASMA CONTND...


3. Menghambat Kerja Mediator yg Dilepaskan sel
Mast
Inhibitor Leukotrien

Antagonis R/ Leukotrien (LT1)


Zafirlukast
Montelukast

Inhibitor Lipoxygenase
Zileuton

AH1

OBAT PILEK (DEKONGESTAN)


MK: agonis R/ vasokonstriksi mukosa & sekresi

Lokal/ Nasal
Spray: dewasa
Drops: < 6 th

Sistemik/ Oral
Pseudoephedrine
PPA
Phenylephrine

AH1

Gen 1
Diphenhydrami
ne
Chlorphenirami
ne
Promethazine
Cyproheptadin
e
Clemastine
Bisulepin

- hidung longgar

Gen 2
Cetirizine
Loratadin
e
Terfenadin
Astemizol

Ephedrine 0,25%
Naphazoline HCl 0,05%
Oxymetazoline 0,025. 0,05%
Phenylephrine
Xylometazoline HCl 0,025. 0,1%

MK:

prod sekret

OBAT BATUK

1. Antitusif
MK: menekan refleks batuk
perifer
Uap menthol, miny.
Eucaliptus
Anestesi lokal topikal
(benzocaine, lidocaine)
Benzonatate

central

Opioid
Codeine
Morphine
Hydrocodon
e

Non Opioid
DMP
(Dextromethorphan)

OBAT BATUK CONTND

2. Ekspektoran
MK: mengencerkan sekret merangsang pengeluaran sekret

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

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

OBAT ANTINYERI,
ANTI-INFLAMASI,
ANTIPIRETIK

MEKANISME NYERI
STIMULUS

analgesik non
narkotik
NSAID
Antiinflamasi
steroid

KERUSAKAN JARINGAN
Transduksi

nestesi lokal

Transmisi

Modulasi

MEDIATOR NYERI
SARAF SENSORIS

(HISTAMIN,PG,BRADIKININ,LEOKOTRIEN,SEROTONIN DLL)
Analgesik
narkotik Persepsi
Anestesi umum

MEDULA SPINAL

RESEPTOR NYERI ( (nociceptor)


THALAMUS / KORTEKS PUSAT NYERI

Tx overdosis opioid

Non Opioid

Acetaminophe
n
Tramadol

COX-1
Inhibitor

COX-2
Inhibitor
Celecoxib
Rofecoxib
Valdecoxib

OBATANESTESI LOKAL
OBAT

DURASI

MAX

1 jam
1-2 jam
1-2 jam
1-2 jam
5-7 jam
6-8 jam

1000 mg
500 mg
500 mg
500mg
200 mg

ester

Prokain, tetracaine, cocaine


2-4%
Lidokain
1-2%
amida
Mepivacaine
1-2%
Prilokain
1-2%
Bupivakain
0,5%
(Levobupivakain) Chirokain
Ropivakain (Naropin)
2,5-7,5%

Obat Migraine
severity

last

mild Migraine

<2 hours

Headache

TTT

analgesics (Aspirin,
Acetaminophen , NSAIDS ) ,
Antiemetic

5HT 1D agonist

Moderate Migraine
<4 hours

Headache

Partial agonist & 5HT

Severe Migraine
Migraine
Headache
Headache
status
migrainosus

over 72 hours

refractory to above

give Antiemetic , analgesics ,


Triptan agents .
refractory to above
Emergency
ttt
give Other
Antiemetic
,
Serotonin Agonist
(Dihydroergotamine , Triptans)

ANTI-GOUT

ANTIHIPERTENSI

JNC 7:

New Blood Pressure Classification

Blood Pressure Classification


SBP* DBP*
(mm Hg)
Normal
<120 and <80
Prehypertension
120-139 or 80-89
Stage 1 hypertension
140-159 or 90-99
Stage 2 hypertension
160 or 100

Bagaimana Terapi Hipertensi ?

stop
merokok
Terapi Non farmakologis : Life style modification
diet : kurangi makanan berlemak & asupan garam,

tambah suplemen ion K, Ca, Mg


menurunkan BB
aktivitas fisik / OR
relaksasi (kurangi stress)

Terapi Farmakologis : Obat antihipertensi

Penggolongan antiHT
CCB
Vasodilator

Nifedipine, verapamil, diltiazem


Oral

Melepaskan NO: hydralazine


Membuka kanal K+: minoxidil

Parenteral

Melepaskan NO: nitroprusside


Membuka kanal K+: diazoxide

ACEI
Diuretik

Captopril, enalapril, quinapril, ramipril


Thiazid: HCT (hydrochlorothiazide) chlorthalidone
Loop Diuretik: furosemide, torsemide, bumetanide
DHK+: amiloride, triamterene, spironolactone

ARB

Irbesartan, losartan, valsartan

Simpatolitik
agents

CNS

Aktivasi reseptor 2: clonidine,


guanabenz, guanfacine
Membentuk neurotransmiter
palsu: methyldopa

Ganglion
otonom
Ujung
saraf

Blok R/ Nikotinik: hexamethonium


Menghambat transpor NE ke vesikel
sinaps: reserpine
Mengosongkan & memblok pelepasan
NE dari tmp penyimpanannya:
guanethidine

R/ Adrenergik

1 blocker: prazosin, oxazosin, terazosin


1 blocker: atenolol, metoprolol
blocker: propranolol

ANTIDIABETIK

PRINSIP PENATALAKSANAAN DM
Pengaturan diet

Minum air banyak, susu skim dan minuman berkalori


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

Farmakoterapi
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Oral Antidiabetics
Ada 5 kelompok :
A. Sulfonylureas
B. Meglitinide
C. Biguanid
E. Alpha-glucosidase inhibitor
D. Glitazone

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Mekanisme kerja
Oral Antidiabetics (OAD)
Me absorbsi glukosa : acarbose, biguanid
Me
sekresi insulin (secretagogues) :
sulfonilurea 1st, 2nd ,3rd , meglitinide
Me produksi glukosa hepar : biguanid
sulfonilurea
Me uptake
di perifer
:
2ndglukosa
, 3rd , biguanid,
thiazolidindion

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ANTIBIOTIK

ANTIBAKTERI
Menghambat sintesis dinding sel

Merusak membran plasma

Menghambat sintesis protein

Menghambat sintesis as nukleat


(Penghambat Girase/ Kuinolon)
Menghambat sintesis metabolit
esensial

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

Polipeptida: tirosidin, gramisidin,


polymyxin, bacitracin
Polien: nystatin, amphotericin B
Aminoglikosida: 30S, 50S
Tetrasiklin: tetracycline, oxytetracycline,
chlortetracycline, rolitetracycline,
demeclocycline, doxycycline, minocycline
Linkosamid: clindamycin, lincomycin
Makrolid: erythromycin, josamycin,
spiramycin, roxithromycin, Clarithromycin
Sulfonamid: sulfacarbamid,
sulfamethoxazole, sulfalen, sulfasalazine
Diaminobenzilpirimidin: trimethoprim,
tetroxoprim, pyrimethamine

Penisilin

laktam

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

Sefalosporin

Generasi 2: cefamandole, cefumaxime,


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

Karbapenem

Imipenem, meropenem

Monobaktam

Aztreonam

Aminoglikosida
30S: streptomycin, neomycin, gentaycin, kanamycin, amikacin, sisomycin,
tobramycin, spectinomycin
50S: (chloramphenicol, azidamphenicol, tiamphenicol), fusidic acid

Menghambat sintesis as nukleat


(Penghambat Girase/ Kuinolon)

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

ANTIMIKOTIK/ ANTIFUNGAL
Membrane disrupting agents

Amphotericin B, Nystatin

Ergosterol syn inh

Nucleic acid inh

Flucytosine

Imidazol: clotrimazole, miconazole, ketoconazole


Triazol: fluconazole, itraconazole
Alilamin: naftifine
Tiokarbamat: tolnaftate
Morfolin: amorolphylline

Antimitotic (spindle disruption)

Griseofulvin

Antiamoeba
Nitroimidazol

Metronidazole, tinidazole

Antiviral
Antiherpes

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 Malang
Praktek
: Jl. Rasuna Said 1 Malang . Telp : 348110
Jam
: 17.00 19.00

Inscripti
o

Malang, 12 11 2007
R/ Methampyron ........................ 500 mg.
Diazepam ............................... 2 mg.
Coffein ................................... 20 mg.
Vit B1 ..................................... 50 mg.

Prescriptio

Mf . la pulv . da in caps dtd . No . XII.


S 1 dd caps . I

Signatura

P.P
Pro
: Tn. Dody
Alamat :

BB :
Umur :

Subscriptio

50

Obat Luar

PULVERES

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