TUGAS BIOFARMASETIKA 1

METABOLISME

NAMA
NO BP
KELAS

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YULIANO MEDORA
1201169
REGULER
STIFARM PADANG
2013

METABOLISM
The purpose of drug metabolism is such that its conversion
is easily excreted kidney, in this case making it more
hydrophilic.
In general, the drug is metabolized by microsomal enzymes
in the endoplasmic reticulum of liver cells. In the process of
metabolism of drug molecules can change the nature of,
among others, become more polar. More polar metabolites
that become insoluble in fat so easily excreted through the
kidneys. Drug metabolites can be more active than the drug
origin (bioaktivasi), no or less active (bio-detoxification or
inactivation) or similar activities.

 Drugs that have been absorbed by the intestine

into the circulation, will be transported through
the portal system of vessels (veins portae), which
is the main blood supply of the stomachintestinal area to the liver. With sublingual
administration, transcutaneous, parenteral or
rectal, the portal system and the liver can be
avoided

 In the liver, and previously also in the

gastrointestinal tract, the whole or part of a drug
that chemical changes in enzymatic and in
general, results perubahannnya (metabolites)
becomes more or less active. This process is also
called detoxification or bioinaktivasi (first pass
effect). There are also drugs that actually
strengthened their pharmacological properties
(bio-activation). Therefore, the metabolic
reactions in the liver and some other organs,
more appropriately called: biotransformation.

 Examples of drugs that become more active by

biotransformation:
- Cortisone and prednisone: cortisol and
prednisolone
- Fenasetin and klorahidrat: paracetamol and
trikloretanol.
metabolite with activity similar
- Chlorpromazine, ephedrine and many
benzodiazepine compounds

Factors affecting the rate of drug biotransformation

1.Concentration
Biotransformation speed will increase when the
concentration of the drug increased.
This is true up to a point where the
concentration becomes so high that
around the enzyme molecule that make changes
continuously occupied by
drug molecules, allows for biotransformation
constant velocity is reached.

2. liver function
on impaired liver function, metabolism may be
faster or slower, allows for the effects of the drug
will be l3. age
in newborns, all liver enzymes have not fully
formed, so that the reaction is slower
metabolism. To avoid overdose, drug dosage
needs to be lowered. Instead there were
metabolically pd obat2xan anak2x lasted llebih
fast, antiepileptic drugs such as phenytoin,
phenobarbital, carbamazepine emah or stronger.

3. elderly
suffered a setback in many processes fisiologisa
al: Renal function, liver enzim2x reduced,
causing delays pervasive biotransformation,
which often affects poisoning
4. Genetic factors: there are people who do not
have certain genetic factors, eg. Enzymes for
sulfadiazine acetylation, consequently reshuffle
this drug to be slow.

5. Use of other drugs

many lipophilic drugs that are able to stimulate
the formation and activation of liver enzymes.
This is called enzyme induction, and which
inhibits the enzyme called enzyme inhibitors

Filtrasi glomerulus
To glomerular filtration, the solubility properties of
the drug had no effect, fat-soluble compounds, difltrasi
as well as water-soluble compounds. Only drugs that
undergo filtration.
Drugs and their metabolites which dissolved in the
plasma across the walls of the ultrafiltrate passively
glomeruli. During the filtrate was concentrated in
tubules, lipophilic substances diffuses back passively
through the cell membrane into the blood, and thus
avoid excretion.

 hydrophilic substances almost immediately

didifusi back and removed through the urine.
Glomerular filtration rate increases in:
- Increase in blood pressure in the glomerular
capillary
- The increase in surface area of glomerular
filtration in quiet conditions.
-The reduction due to reduced plasma protein
binding protein
the drug substance

Reabsorpsi tubulus
tubular reabsorption, for most of the ingredients
will be reabsorbed through passive diffusion
process, and depends on:
- The nature of drug solubility
compounds that are soluble in fat and well
absorbed dg intestine, also easily penetrates the
epithelial tubule and reabsorbed well, on the
contrary, hydrophilic compounds that can hardly
be absorbed by the intestine, it is difficult to
diffuse through the tubules.

urine pH prices
dieksresi strong weakly basic price reduction of
urinary pH, weak acids dieksresi strong price
increase urine pH (changes into a soluble salt
form. Oki on intoxication with alkaline material
ie. Alkaloids, elimination of toxins can be
accelerated with acidified urine and intoxication
with acid substance , such as barbiturates acid,
elimination can be accelerated by pembasaan
urine.

 In addition to acids, organic bases can also be

actively secreted from tubular cells with the help
of enzymes pengankut. Kadang2x there is
competition between several ions to the
enzymes. For example: probenecid compete for
enzymes penisislin pengankutnya, to antibiotic
excretion slowed and its effects are longer.

 Acid / base transporters and enzymes work

sendiri2x, and ill depend on each other.
The dose is too high or too frekuen can cause
toxic effects, whereas the dose is too low or too
seldom produces no effect, even in
chemotherapeutic resistance can cause germs.

 Drugs with a long half-life, over 24 hours, is

generally given enough doses (maintenance)
once daily, do not need to be up to 2-3 times a
day, for example digoxin.
Conversely, a drug that is metabolized quickly
and t1 / 2 of her short, should be given up to 3-6
times a day so that plasma levels remain high.

 excretion of a drug and its metabolites:

concentrations causing a decrease in the body of
nutritious ingredients.
excretion can occur depend on:
physicochemical properties: molecular weight,
pK a, solubility, vapor pressure.

 excretion can take place through:

- Skin: concurrent with sweat, eg, paraldehyde,
bromide
- Ation: drug and its metabolites are excreted mll
ation interchangeable and interchangeable harm
the baby pd (poisoning), for example; sleeping
pills, nicotine, penicillin, chloramphenicol, INH,
ergotamine
- Kidney (urine)
- Bile and gut (feces)
- Lung (with expiratory air)

Elimination through the kidneys

Kidney is an important organ of excretion.
Most drugs are excreted through the urine, and
the prevalence of each drug in the form of
metabolites excreted, and only a small part in
the original state.
Zat2x in an ion which is easily soluble in urine,
excreted

 Substances that lipophilic and unionized,

slower excretion, to improve the properties of
hidrofilnya, then the biotransformation included
group-OH or-COOH and into the molecule.

 The speed and magnitude of excretion through

the kidney is determined by:
- Glomerular filtration
- Tubular reabsorption
- Tubular secretion