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Dr. Asra Hameed
Pharm.D (JUW)
asra_hameed1@hotmail.com
Category:
Anti-infective
drugs
Antibiotics,
systemic
Anti-
tuberculosis
drugs
Overview
Isoniazid is the hydrazide of isonicotinic acid.
Isoniazid is structurally similar to pyridoxine and
introduced in 1952.
It is the most active drug for the treatement of
tuberculosis caused by susceptible strains used
either alone or in combination with other drugs.
It is prepared by chemical synthesis.
It is available in combination with pyrazinamide,
rifampicin, ethambutol, pyridoxine and
cyanocobalamine.
Isoniazid also known as Isonicotic Acid Hydrazide, Isonicotic Acid
Hydrazide, Isonicotic Acid Hydrazide. .
It is of Synthetic origin and belongs to Hydrazine.
It belongs to Antimycobacterial agent pharmacological group on the
basis of mechanism of action and also classified in Antituberculous
Drugs pharmacological group.
The Molecular Weight of Isoniazid is 137.10.
Its pKa is 1.8, 3.5, 9.5.
MOA: Isoniazid inhibits synthesis of
mycolic acids, which are essential
components of mycobacterial cell walls.
Oral
absorpti
on of
Isoniazi
d is
found to
be
95.5%
±4.5
Metabol
ism is
reported
Hepatic
&
Intestin
al.
Indications
Acute
leukemia
Mycobacteri
al infection
Prophylaxis
of TB
Tuberculosis
Vestibular
disorders
An
alternative
drug of
choice
in Pulmonar
y TB
Diabetes
mellitus
Hyper
sensitivi
ty
Seizures
Drug
Interactions
Alcohol
Alcohol
Alprazolam
Aluminium
Hydroxide and
Oxide
Bovine Insulin
Bromazepam
Calciferol
Carbamazepine
Chlorzoxazone
Drug
Interactions
Cycloserine
Diazepam
Digitoxin
Disulfiram
Enflurane
Estazolam
Ethionamide
Ethosuximide
Ethosuximide
Fosphenytoin
Gestodene
Human Insulin
Insulin Glulisine
Drug
Interactions
Isophane insulin
Ketoconazole
Magnesium
Oxides and
Hydroxides
Metformin (HCl)
Paracetamol
Paroxetine
Phenytoin (Na)
Podophyllum
Porcine Insulin
Prednisolone
Primidone
Drug
Interactions
Prothionamide
Pyrazinamide
Pyridoxine
Rifampicin
Rifampicin
Salicylamide
Sevoflurane
Stavudine
Tacrolimus
Triazolam
Zalcitabine
Zalcitabine
Ziprasidone
Zolpidem
False positive
result of urine
in diabetics
using clinitest.
Side Effects
Hepatotoxicity,
Pancreatitis,
Lupus erythematosus,
Peripheral neuropathy,
Gynecomastia,
Increase liver enzyme,
Hepatitis,
Nausea,
Vomiting,
Tachycardia,
Convulsions,
Coma,
Seizures,
Urinary retention,
Dizziness,
Hyperreflexia,
Slurred speech,
Diarrhea,
Fever,
Skin eruptions,
Vasculitis,
Skin eruptions,
Skin rashes
Dosage
Adult Dosage Single
Dose
Frequency Route Instructions
300 mg
Paedriatic
Dosage ( 20 Kg.
)
Single Dose Frequency Route Instructions
15 mg/kg 15 (15) 24 hourly Intra Muscular Single Dose
10 mg/kg 10 (10) 24 hourly Intra Venous Single Dose
Neonatal Dosage
( 3 Kg. ) Single Dose Frequency Route Instructions
10 to 15 mg/kg 12 (12.5) 24 hourly Intavenous
10 to 15 mg/kg 12 (12.5) 24 hourly Intramuscular
10 to 15 mg/kg 12 (12.5) 24 hourly Oral
High Risk Groups
• Kidney dysfunction, Liver Malfunction, and
Neonates.
Warning / Precautions
• Minimize alcohol consumption
• Used with caution if patients have kidney or liver
problems, diabetes, history of alcohol use and of
any drug allergy.
• Avoid With Tyramine and Histamine-containing
foods e.g. fish, cheese, yeast extract or sausages.
• It should be used during pregnancy or lactation
only if clearly needed.
Storage Conditions
Oral Syrup, Inj
Store at room temperature. Do
not Freeze. Protect from
Sunlight.
Tab
Store in a well closed container,
Between 15°C-30°C. Protect
from Sunlight and Moisture.
Manufacturer(s) of Isoniazid in Pakistan.
Abbott
Adamjee
Amson
CCL
Dosaco
Efroze
Ferro
Genera
Genix
Geofman
Gray's
Irza
Jawa
Jinnah
LCPW
Lisko
Lowitt
Nabiqasim
Noa Hemis
Novartis
Pacific
PDH
Pfizer
Pharmacare
Pharmawise
Polyfine
Reko
Rex
Saydon
Sharex
Standard
Syntex
Unexo
Wilshire
Zafa
Zaka
Available brands and strengths in Pakistan.
Single Ingrediant
Syrup :50 mg 50 mg/5ml
Tabs: 50 mg 100 mg 300 mg 400
mg
Multi Ingrediant
Syrup: 50 mg/5ml 60 mg/5ml
Sachet: 30 mg
Paed Tab : 60 mg
Tabs: 30 mg 50 mg 60 mg 75 mg
80 mg 100 mg 150 mg 300 mg
Caps :150 mg
FAIRZIDE
I.N.H
ISONIAZID
ISONIAZIDE
ISOZIDE TABLET
NIAZID
NYDRAZIDE
PHAROZIDE
REMONIAZID
SONOREX
Pyrazinamide, the pyrazine
analogue of nicotinamide, is
an antituberculosis agent.
It is a white crystalline
powder.
Sparingly soluble in water.
Pyrazinamide is an antibiotic treats only bacterial infection.
It will not work for viral infections (such as common cold,
flu).
It is an antibiotic and works by stopping the growth of
bacteria.
Pyrazinamide is a drug used to treat tuberculosis. The
drug is largely bacteriostatic, but can be bacteriocidal.
Pyrazinamide is only used in combination with other drugs
such as isoniazid and rifampicin in the treatment of
Mycobacterium tuberculosis.
Rapid and almost complete from GI tract. T
max is within 2 h and plasma concentrations
range from 30 to 50 mcg/mL.
Widely distributed to most fluids and
tissues, including the liver, lungs, kidney,
and bile. Excellent penetration into CSF
(87% to 105%). Vd is 0.57 to 0.74 L/kg.
Protein binding is approximately 10%.
Distributes into breast milk.
Renal (3% as unchanged form.70% of
orally adminsitered dose is excreted in the
urine. The t ½ is approximately 1.6hr.
ADULTS
• PO 15 to 30 mg/kg every day or 50 to 70
mg/kg 2 times/wk.
CHILDRE
N
• PO 15 to 30 mg/kg every day or 50 to 70
mg/kg 2 times/wk
ADMINIST
R
ATION
• Administer without regard to meals.Administer
with food if GI upset occurs.
STORAG
E/STABLI
TY
• Store at room temperature (59° to 86°F) in
tightly closed, light-resistant container.
M
A
L
A
I
S
E
U
R
T
I
C
A
R
I
A
P
R
U
R
I
T
I
S
D
Y
S
U
R
I
A
A
N
O
R
E
X
I
A
S
O
B
(DIFFICULTY
IN
BREATHING)
S
W
E
L
L
I
N
G
SEVERE
D
I
Z
Z
I
N
E
S
S
YELLOWING
OF
SKIN
AND
EYES
UNUSUAL
BRUISING
AND
BLEEDING
ARTHRALGIA: Mild
joint or muscle pain /
tenderness.
Pyrazinamide is a prodrug that stops the growth of Mycobacterium
tuberculosis.
Pyrazinamide diffuses into M. tuberculosis, where the enzyme
pyrazinamidase converts pyrazinamide to the active form pyrazinoic
acid.
Under acidic conditions, the pyrazinoic acid that slowly leaks out
converts to the protonated conjugate acid, which is thought to diffuse
into the bacilli and accumulate.
The net effect is that more pyrazinoic acid accumulates inside the
bacillus and was thought to inhibit the enzyme fatty acid synthase
(FAS) , which is required by the bacterium to synthesise fatty acids,the
accumulation of pyrazinoic acid disrupts membrane potential and
interferes with energy production, necessary for survival of M.
tuberculosis at an acidic site of infection.
Pyrazinoic acid and its ester inhibit the synthesis of fatty
acids.Pyrazinoic acid binds to the ribosomal protein S1 (RpsA) and
inhibits trans-translation.
It shows the ability of the drug to kill dormant mycobacteria.
CONTRAINDICATIONS
ACUTE GOUT
SEVERE HEPATIC
DAMAGE
HAVE SHOWN
HYPERSENSITIVITY
TO IT
Avonex Prefilled Syringe
Betaseron black cohosh
Amersham Indium (111In) Oxine
Avonex Pen bedaquiline
Adcetris (brentuximab)v
Atripla Avonex
Avonex (interferon beta-1a)
vonex Pen (interferon beta-1a) Avonex Prefilled Syringe
Amersham Indium (111In) Oxine
Atripla
Tice BCG Vaccine (bcg)
Adcetris (brentuximab)
teriflunomide
TheraCys (bcg) Tice BCG (bcg)
Rifamate
Rifater Rimactane
mipomersen
Rifadin Rifadin IV
Kynamro (mipomersen)
leflunomide lomitapide
IsonaRif
isoniazid / rifampin Juxtapid (lomitapide)
Arava (leflunomide)
Aubagio (teriflunomide) bcg
Rheumatrex Dose Pack
Sandimmune Sirturo
Rebif
Rebif Rebidose Revia
peginterferon beta-1a
Plegridy Rasuvo
Otrexup
Pharmorubicin PFS Pharmorubicin RDF
Methotrexate LPF Sodium
naltrexone Neoral
indium oxyquinoline in-111
methotrexate morphine
idelalisib
interferon beta-1a interferon beta-1b
Extavia
Folex PFS Gengraf
Ellence
Embeda epirubicin
Depade
efavirenz tenofovir
Clolar
Contrave cyclosporine
brentuximab
bupropion clofarabine
Aloprim
allopurinol
Trexall
Tabloid
Lopurin
Zydelig
Vivitrol
thioguanine
Sustiva
Zyloprim
Ibuprofen to a class of drugs called NON-STEROIDAL
ANTIINFLAMMATORY DRUGS (NSAIDS).
BRANDS:
Advil
Medipren
Motrin
Nuprin
Pedia care fever etc
Ibuprofen is a non selective inhibitor of an enzyme called
Cyclooxygenase (COX), which is required for the synthesis of
Prostaglandins via the arachidonic acid pathway.
COX is needed to convert arachidonic acid to
prostaglandins H2 (PGH2) in the body.
The PGH2 is then converted to
prostaglandins.
The inhibition of COX by ibuprofen
therefore lowers the level of
prostaglandins made by the body.
Treat minor aches & pain
caused by the common cold
Headache
Toothache
Back or muscle ache
Arthritis
Also used to reduce fever
Ibuprofen is contraindicated in patients with
known hypersensitivity to ibuprofen.
It should not be given to patients who have experienced
asthma, urticaria, or allergic type reactions after taking
asprin or other NSAIDS.
It is contraindicated in the setting of coronary artery bypass
graft (CABG) surgery.
It should be avoided in pregnancy.
Is better at reducing fever
than Tylonol.
Its anti- platelet properties
are mild and short lived as
compared to aspirin.
CATEGORY
Anti-infective
drugs
Dermatological
drugs (topical)
Anti-Viral drugs
OVERVIEW
Ribavirin is antiviral agent.
Ribavirin is a synthetic guanosine analogue.
Ribavirin is active against several DNA and RNA viruses.
Ribavirin is administered to infants and young children with respiratory
syncytial virus (RSV) severe chest infections or pneumonia.
Ribavirin also known as
Tribavirin.
It is of Synthetic origin
and belongs to
Triazoribose.
t belongs to Antiviral
Agents pharmacological
group on the basis of
mechanism of action,
The Molecular Weight of
Ribavirin is 244.20.
MOA: May inhibit the initiation and
elongation of RNA fragments by
inhibiting polymerase activity, which in
turn results in the inhibition of viral
protein synthesis
Oral
absorpti
on is
found to
be 45% .
metaboli
sm is
reported
Hepatic
and
Renal.
INDICATIONS
Metastati
c
melanom
a
Treatme
nt of
chronic
Hepatitis
C virus
RSY
infectio
n
Pneumoni
a
Bronchiti
s
Auto immune
hepatitis
&
Haemoglobin
o-pathies
Hyper
sensitivi
ty
Pregnan
cy
Drug Interactions
Ribavirin is known to interact with other drugs, the details of drug interactions
is as follows:
Drug Details
Abacavir
Didanosine Coadministration of Ribavirin and
didanosine is contraindicated as
because exposure to the active
metabolite of didanosine are increased.
Fatal hepatic failure, as well as
peripheral neuropathy, pancreatitis, and
symptomatic hyperlactatemia/lactic
acidosis have been reported in patients
receiving both didanosine and ribavirin.
Interferon Alpha 2b
Stavudine Ribavirin may antagonize the cell culture
antiviral activity of stavudine against HIV.
Zidovudine Ribavirin may antagonize the cell culture
antiviral activity of Zidovudine against
HIV.
SIDE EFFECTS
Thirst symptomaticInsomnia
Headache Fatigue
Metallic
taste adverse
Mood
swings
Decreas
e in RBCreactions
GI
Disturbance
DOSAGE
Dose
Single
Dose
Frequenc
y
Route Instructions
Adult Dosage
400 mg 400 (400) 12 hourly PO For Hapatitis C, for 6 months.
Paedriatic Dosage ( 20 Kg. )
2.5 to 5
mg/kg
3.8 (3.75) 8 hourly Oral For 1-2 Weeks
Neonatal Dosage ( 3 Kg. )
3.125 to
6.25
mg/kg
4.7
(4.6875)
8 hourly Oral
HIGH RISK GROUPS
• Drug should not be given to Pregnant
Mothers, patients suffering from
Kidney dysfunction, and Neonates.
WARNING / PRECAUTIONS
• Ribavirin should not be used during
pregnancy, since the risks outweigh
the benefits. Birth control measures
should be taken while using this
medicine
STORAGE CONDITIONS
Inhalation Soln (freshly
prepared),capsules and
tablets
Store at room temperature..
Protect from Sunlight and
Moisture.
Use within 24 hrs if kept at room
temperature.
AVAILABLE BRANDS
Single Ingredient
• Syrup: 50 mg, 50
mg/5ml, 100 mg/5ml
• Cream: 7.5 %w/w
• Tabs: 200 mg, 400 mg, 500
mg, 600 mg
• Caps: 100 mg, 200
mg, 400 mg, 600 mg
Multi ingredient
• Syrup: 1.31 mg/5ml
• Tabs: 15 mg
• Copegus®
• Rebetol®
• Ribasphere®
• Virazole®
CATEGORY
Anti-malarial
drugs
Anti
protozoals
Anti-
infective
drugs
OVERVIEW
It is a water-soluble hemisuccinate derivative of dihydroartemisinin.
Artesunate and its active metabolite dihydroartemisinin are
potent blood schizonticides, active against the ring stage of
the parasite
It is also active against chloroquine and mefloquine resistant strains
of P. falciparum.
Artesunate is ideal for the treatment of severe malaria, including
cerebral malaria.
It is unstable in neutral solution and is therefore only available for
injections as artesunic acid.
PRIMARY CHARACTERISTICS
It is of Semi Synthetic origin.
The Molecular Weight of Artesunate is
384.42.
Used for oral, rectal, intravenous and intramuscular administration.
MOA
PHARMACOKINETICS
Plasma half life is 45 min
2.4mg/kg dose in adult patients with P. falciparum malaria: Cmax:
11,330 mcg/L; Half-life: 2.7 hours; Volume of distribution: 0.14 L/kg;
INDICATIONS
Artesunate is primarily indicated in conditions like Cerebral
malaria, Chloroquine resistant malaria.
CONTRAINDICATIONS
Artesunate is contraindicated in conditions
like Hypersensitivity,Pregnancy.
DRUG INTERACTIONS
No data regarding the interactions of Artesunate was found.
ADVERSE EFFECTS
•lower reticulocyte counts
•Flatulence,
• Dizziness,
• Headache,
•Delayed haemolysis (occurring
around two weeks after
treatment)
•Vomiting,
• Diarrhea,
•Fever,
• Abdominal pain,
• Rashes
•Itching,
• Hair loss,
•Convulsions.
AVAILABLE BRANDS
Single Ingredient
Inj: 60 mg,
Tabs: 50 mg,
Multi ingredient
Tabs: 25 mg, 50
mg, 100 mg,
DOSAGE
Dose Single Dose Frequency Route Instructions
Adult Dosage
2.4 mg/kg 2.4 (2.4) As
recommended.
IM Severe malaria: This dose is followed by
1.2mg/Kg at 12 and 24 hours then 1.2mg/Kg
daily for 6 days. If the patient can swallow, the
daily dose can be given orally.
2.4 mg/kg 2.4 (2.4) As
recommended.
IV Severe malaria: This dose is followed by
1.2mg/Kg daily until the patient can take orally
artesunate or another effective antimalarial
drug.
4 mg/kg 4 (4) As
recommended.
PO Monotherapy: 4mg/Kg loading dose on the
first day followed by 2mg/Kg once a day for 6
days.
4 mg/kg 4 (4) As
recommended.
PO Combination therapy: 4mg/Kg once a day for
3 days plus mefloqine (15mg or 25mg of base
per Kg) as a single dose or split dose on the
second and/or third day.
Paedriatic Dosage ( 20 Kg. )
No data regarding the Paedriatic dosage details of Artesunate is available.
Neonatal Dosage ( 3 Kg. )
No data regarding the neonatal dosage details of Artesunate is available.
INTERFERENCEIN PATHOLOGY
No data regarding the pathological interferences produced by
artesunate is available
Anti-infective
drugs
Antiprotozoal
drugs
Antimalarial
Amodiaquine is a 4-
aminoquinoline
antimalarial with an
action and uses similar to
that of chloroquine.
Amodiaquine is not
recommended for the
prophylaxis of
malaria.
Amodiaquine is used
to treat malaria
Amodiaquine HCl is the
derivative of Amodiaquine.
It is of Synthetic origin and
belongs to Quinoline Phenol
It belongs to Antiplasmodial
pharmacological group on the
basis of mechanism of action and
also classified in Antimalarial
Agent
pharmacological
group.The Molecular
Weight of Amodiaquine is
464.80.
• The mechanism of
plasmodicidal action of
amodiaquine is not
completely certain. Like
other quinoline
derivatives, it is thought to
inhibit heme polymerase
activity. This results in
accumulation of free
heme, which is toxic to the
parasites. The drug binds
the free heme preventing
the parasite from
converting it to a form less
toxic. This drug-heme
complex is toxic and
disrupts membrane
function.
• Oral absorption of Amodiaquine is found to
be 82.5% ±2.5. Plasma protien binding is
extensive. Presystemic metabolism is noted
to be 82.5% ±2.5 and metabolism is reported
via liver. Plasma half life is 5.2 hr.
INDICATIONS
• Amodiaquine is primarily indicated in
conditions like Malaria, Nephrogenic and
partial pituitary diabetes insipidus.
• Amodiaquine is
contraindicated in
conditions
like Malaria
prophylaxis
DRUG
INTERACTIONS
• No data regarding
the interactions of
Amodiaquine was
found.
• The severe or irreversible
adverse effects of
Amodiaquine, which give
rise to further
complications include
Liver damage.
• Amodiaquine produces
potentially life-threatening
effects which include
Blood dyscrasias, Lupus
erythematosus. which are
responsible for the
discontinuation of
Amodiaquine therapy.
• The symptomatic adverse
reactions produced by
Amodiaquine are more or
less tolerable and if they
become severe, they can
be treated
symptomatically, these
include Weakness,
Nausea, Vomiting,
Diarrhea, Abdominal
cramps, Tinnitus, Irregular
heart beat, Termors,
General malaise, Skin
pigmentation, Palate
pigmentation, Nail-beds
pigmentation.
Dose Single Dose Frequency Route Instructions
Adult Dosage
35 mg/kg 35 (35) As
recommende
d.
PO For 3 days.
Paedriatic Dosage ( 20 Kg. )
5 to 10
mg/kg
7.5 (7.5) As
recommende
d.
Oral Once a Week
Neonatal Dosage ( 3 Kg. )
6.25 mg/kg 6.2 (6.25) As
recommende
d.
oral Once a week
Drug should not be given to
Pregnant Mothers.
• WARNING /
PRECAUTIONS
It should be used with
caution in patients allergic
to peanuts, not to be used
on broken, infectious skin.
It should be used with
caution in blockage of the
gut (intestinal obstruction).
Chemical class: Rifamycin.
Therapeutic class: Anti tuberclosis
agent,antibiotic,antinfective.
Available dosage forms: It is available by mouth
and intravenously.
• Rifampicin inhibits bacterial DNA-dependent
RNA synthesis by inhibiting bacterial DNA-
dependent RNA polymerase.
• Rifampicin is easily absorbed from
the gastrointestinal (GI) tract.
• Only about 7% of the administered drug will be excreted
unchanged through the urine, About 60% to 65% is
excreted through the feces.
The half-life of rifampic in ranges from 1.5 to 5.0 hours.
About 60% to 90% of the drug is bound to plasma
proteins.
Metabolized by liver.
Distribution of the drug is high throughout the body, Since
the substance itself is red, this high distribution is the
reason for the orange-red color of the saliva, tears,
sweat, urine, and feces.
• TUBERCLOSIS.
• ATYPICAL MYCOBACTERIAL INFECTIONS.
• LEPROSY.
• PROPHYLAXIS OF H.INFLUENZA TYPE B
DISEASE IN CHILDERNS.
Contraindicated: in jaundice and porphyria.
Precautions:Liver impairment,imparts organs red
colour to urine,saliva,tears,sweat and
sputum,young childerns,pregnancy,breast
feeding,old age.
• GI:Anorexia,nausea,vomiting,dirrhoea.
• Respiratory symptoms:SOB,collaps and
shock,haemolytic
anaemia,thrombocytpenia,jaundice,flushing,urtic
aria,rash.
• Other ADR:Edema,muscular
weakness,myopathy,leucopenia,eosinophillia,me
nstrual disturbances.
• Rifampicin induce microsomal enzymes and may reduce
the efficacy of following drugs:
• Acetaminophin,oralanticoagulants,barbiturates,BDZ,chlor
amphenicol,oral
contraceptives,corticosteroids,cyclosporin,digoxin,beta
blockers,slphones,theophylline,verapamil.
• Halothane: Hepatotoxicity.
• Isoniazid: Higher incidence of hepato toxicity than alone.
• Ketokonazole: Treatment failure.
• Food: Interfere with absorption of rifampicin,take on
empty stomach.
• ADULTS:
• TUBERCLOSIS:450-600Mg po.
• MENI NGITS:600mg bid for 2 days.
• H.INFLUENZA:20Mg/kg daily for 4 days.
• BRUCILLOSIS:600-1200Mg daily.
• CHILDERNS:
• TUBERCLOSIS:10-20Mg/kg/day po.
• MENINGITIS:Under 3 months-1 year 5mg/kg bid for 2
days.
• H.INFLUENZA:10Mg/kg for 4 days.
Antibiotic Anti
tubercular
Anti
Bacterial
Amikacin sulfate is a semi-synthetic
amino glycoside antibiotic.
It is used to treat different types of bacterial
infections.
Amikacin is most often used for treating severe,
hospital-acquired infections
• Inhibit Protein
synthesis by binding
directly to the
30S ribosomal subunit
• causing misreading
of mRNA and leaving
the bacterium unable
to
synthesize proteins vit
al to its growth.
• Absorption: IM: May be delayed in
bedridden patient
• Volume of distribution: 0.25-0.4 L/kg,
primarily into extracellular fluid (highly
hydrophilic); penetrates blood-brain barrier
when meninges inflamed; crosses
placenta.
• Excretion: urine (94-98%)
• Half-Life: 2-3 hr Peak Plasma Time: IM:
45-120 min
• Protein Binding: 0-11%
 Central nervous
system
 Biliary and intestinal
infection
 Intraabdominal
infections
 Secondary infection
after combustion
 Infections of bones
and joints.
:
 Patients
hypersensitive to drug
or other amino
glycosides.
 Pregnancy
Breast feeding
 Impaired renal
function.
 Neuromuscular
disorders.
Amdinocilin
Amoxicilin
Benzylpenicillin
Cefixime
Digoxin
Furosemide
Ibuprofen
Neproxin
Pipercillin
Vancomycin
Adult dose for
bacteremia:
Adult Dose
for Pneumonia:
Adult Dose
for Nosocomial Pneumoni
a:
•15 to 22.5 mg/kg/day
IV or IM in 1 to 3divided
doses,
•(initial maximum of 1.5
g/day, then adjust dose
based on desired serum
levels
•5 to 22.5
mg/kg/day IV or IM in 1
to 3divided doses.
•(initial maximum of 1.5
g/day, then adjust dose
based on desired serum
levels
•20 mg/kg /day IV
in 1to 3 divided doses
• Ototoxicity
• Neurotoxicity-
Neuromuscular Block
age
• Nephrotoxicity:
• Other:
• skin
• Rash ,headache
,nausea and vomiting,
eosinophilia
and hypotension
Cycloserine is a second-line, broad-spectrum
antibiotic, produced by Streptococcus orchidaceus.
In 1955, it was first isolated from a fermentation brew
and was later synthesized.
Cycloserine is used in the treatment of active
pulmonary and extrapulmonary tuberculosis (TB),
when primary agents have failed (such as INH,
rifampin, streptomycin etc).
When Cycloserine is employed to treat tuberculosis,
it must be given together with other effective agents.
Cycloserine is given orally. It was approved by the
FDA in 1956.
Category:
Anti-
infective
drugs
Antibiotics, systemic
Anti-
tuberculosis
drugs
Cycloserine is an analog of the amino
acid D-alanine. It interferes with an
early step in bacterial cell wall
synthesis in the cytoplasm by
competitive inhibition of two enzymes,
L-alanine racemase, which forms D-
alanine from L-alanine, and D-
alanylalanine synthetase, which
incorporates D-alanine into the
pentapeptide necessary for
peptidoglycan formation and bacterial
cell wall synthesis.
• Used in combination with up to
5 other drugs as a treatment
for Mycobacterium avium
complex (MAC) and is also
used to treat tuberculosis (TB)
Indication
• Cycloserine is contraindicated
in conditions like Epilepsy,
Renal failure, Hypersensitivity,
Mental illness.
Contraindicated
• Oral absorption of Cycloserine is found to be 50%
±50.
• Plasma protien binding is < 20%.
• Presystemic metabolism is noted to be 5% ±5 and
metabolism is reported hepatic.
• Renal Excretion accounts for 50-70% (unchanged)
and plasma half life is 10 hr.
Pharmacokinetics
• Congestive heart failure, Psychiatric disturbances,
Megaloblastic anemia, Excitement, Convulsions,
Nervous system manifestation, Vertigo, Headache,
Drowsiness, Irritability, Nausea, Fever, Anxiety,
Rashes, Confusion, Photosensitivity, Depression,
Cardiac arrhythmias, Tremor, Disorientation,
Peripheral neuropathy, Aggression, Hyper-reflexia,
Confusion, Suicidal tendencies.
Side Effects
hospital pharmacy

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hospital pharmacy

  • 1. Dr. Asra Hameed Pharm.D (JUW) asra_hameed1@hotmail.com
  • 2.
  • 4. Overview Isoniazid is the hydrazide of isonicotinic acid. Isoniazid is structurally similar to pyridoxine and introduced in 1952. It is the most active drug for the treatement of tuberculosis caused by susceptible strains used either alone or in combination with other drugs. It is prepared by chemical synthesis. It is available in combination with pyrazinamide, rifampicin, ethambutol, pyridoxine and cyanocobalamine.
  • 5. Isoniazid also known as Isonicotic Acid Hydrazide, Isonicotic Acid Hydrazide, Isonicotic Acid Hydrazide. . It is of Synthetic origin and belongs to Hydrazine. It belongs to Antimycobacterial agent pharmacological group on the basis of mechanism of action and also classified in Antituberculous Drugs pharmacological group. The Molecular Weight of Isoniazid is 137.10. Its pKa is 1.8, 3.5, 9.5.
  • 6. MOA: Isoniazid inhibits synthesis of mycolic acids, which are essential components of mycobacterial cell walls.
  • 7. Oral absorpti on of Isoniazi d is found to be 95.5% ±4.5 Metabol ism is reported Hepatic & Intestin al.
  • 10. Drug Interactions Alcohol Alcohol Alprazolam Aluminium Hydroxide and Oxide Bovine Insulin Bromazepam Calciferol Carbamazepine Chlorzoxazone Drug Interactions Cycloserine Diazepam Digitoxin Disulfiram Enflurane Estazolam Ethionamide Ethosuximide Ethosuximide Fosphenytoin Gestodene Human Insulin Insulin Glulisine Drug Interactions Isophane insulin Ketoconazole Magnesium Oxides and Hydroxides Metformin (HCl) Paracetamol Paroxetine Phenytoin (Na) Podophyllum Porcine Insulin Prednisolone Primidone Drug Interactions Prothionamide Pyrazinamide Pyridoxine Rifampicin Rifampicin Salicylamide Sevoflurane Stavudine Tacrolimus Triazolam Zalcitabine Zalcitabine Ziprasidone Zolpidem
  • 11. False positive result of urine in diabetics using clinitest.
  • 12. Side Effects Hepatotoxicity, Pancreatitis, Lupus erythematosus, Peripheral neuropathy, Gynecomastia, Increase liver enzyme, Hepatitis, Nausea, Vomiting, Tachycardia, Convulsions, Coma, Seizures, Urinary retention, Dizziness, Hyperreflexia, Slurred speech, Diarrhea, Fever, Skin eruptions, Vasculitis, Skin eruptions, Skin rashes
  • 13. Dosage Adult Dosage Single Dose Frequency Route Instructions 300 mg Paedriatic Dosage ( 20 Kg. ) Single Dose Frequency Route Instructions 15 mg/kg 15 (15) 24 hourly Intra Muscular Single Dose 10 mg/kg 10 (10) 24 hourly Intra Venous Single Dose Neonatal Dosage ( 3 Kg. ) Single Dose Frequency Route Instructions 10 to 15 mg/kg 12 (12.5) 24 hourly Intavenous 10 to 15 mg/kg 12 (12.5) 24 hourly Intramuscular 10 to 15 mg/kg 12 (12.5) 24 hourly Oral
  • 14. High Risk Groups • Kidney dysfunction, Liver Malfunction, and Neonates. Warning / Precautions • Minimize alcohol consumption • Used with caution if patients have kidney or liver problems, diabetes, history of alcohol use and of any drug allergy. • Avoid With Tyramine and Histamine-containing foods e.g. fish, cheese, yeast extract or sausages. • It should be used during pregnancy or lactation only if clearly needed.
  • 15. Storage Conditions Oral Syrup, Inj Store at room temperature. Do not Freeze. Protect from Sunlight. Tab Store in a well closed container, Between 15°C-30°C. Protect from Sunlight and Moisture.
  • 16. Manufacturer(s) of Isoniazid in Pakistan. Abbott Adamjee Amson CCL Dosaco Efroze Ferro Genera Genix Geofman Gray's Irza Jawa Jinnah LCPW Lisko Lowitt Nabiqasim Noa Hemis Novartis Pacific PDH Pfizer Pharmacare Pharmawise Polyfine Reko Rex Saydon Sharex Standard Syntex Unexo Wilshire Zafa Zaka
  • 17. Available brands and strengths in Pakistan. Single Ingrediant Syrup :50 mg 50 mg/5ml Tabs: 50 mg 100 mg 300 mg 400 mg Multi Ingrediant Syrup: 50 mg/5ml 60 mg/5ml Sachet: 30 mg Paed Tab : 60 mg Tabs: 30 mg 50 mg 60 mg 75 mg 80 mg 100 mg 150 mg 300 mg Caps :150 mg FAIRZIDE I.N.H ISONIAZID ISONIAZIDE ISOZIDE TABLET NIAZID NYDRAZIDE PHAROZIDE REMONIAZID SONOREX
  • 18.
  • 19. Pyrazinamide, the pyrazine analogue of nicotinamide, is an antituberculosis agent. It is a white crystalline powder. Sparingly soluble in water.
  • 20. Pyrazinamide is an antibiotic treats only bacterial infection. It will not work for viral infections (such as common cold, flu). It is an antibiotic and works by stopping the growth of bacteria. Pyrazinamide is a drug used to treat tuberculosis. The drug is largely bacteriostatic, but can be bacteriocidal. Pyrazinamide is only used in combination with other drugs such as isoniazid and rifampicin in the treatment of Mycobacterium tuberculosis.
  • 21. Rapid and almost complete from GI tract. T max is within 2 h and plasma concentrations range from 30 to 50 mcg/mL. Widely distributed to most fluids and tissues, including the liver, lungs, kidney, and bile. Excellent penetration into CSF (87% to 105%). Vd is 0.57 to 0.74 L/kg. Protein binding is approximately 10%. Distributes into breast milk. Renal (3% as unchanged form.70% of orally adminsitered dose is excreted in the urine. The t ½ is approximately 1.6hr.
  • 22. ADULTS • PO 15 to 30 mg/kg every day or 50 to 70 mg/kg 2 times/wk. CHILDRE N • PO 15 to 30 mg/kg every day or 50 to 70 mg/kg 2 times/wk ADMINIST R ATION • Administer without regard to meals.Administer with food if GI upset occurs. STORAG E/STABLI TY • Store at room temperature (59° to 86°F) in tightly closed, light-resistant container.
  • 24. Pyrazinamide is a prodrug that stops the growth of Mycobacterium tuberculosis. Pyrazinamide diffuses into M. tuberculosis, where the enzyme pyrazinamidase converts pyrazinamide to the active form pyrazinoic acid. Under acidic conditions, the pyrazinoic acid that slowly leaks out converts to the protonated conjugate acid, which is thought to diffuse into the bacilli and accumulate. The net effect is that more pyrazinoic acid accumulates inside the bacillus and was thought to inhibit the enzyme fatty acid synthase (FAS) , which is required by the bacterium to synthesise fatty acids,the accumulation of pyrazinoic acid disrupts membrane potential and interferes with energy production, necessary for survival of M. tuberculosis at an acidic site of infection. Pyrazinoic acid and its ester inhibit the synthesis of fatty acids.Pyrazinoic acid binds to the ribosomal protein S1 (RpsA) and inhibits trans-translation. It shows the ability of the drug to kill dormant mycobacteria.
  • 26. Avonex Prefilled Syringe Betaseron black cohosh Amersham Indium (111In) Oxine Avonex Pen bedaquiline Adcetris (brentuximab)v Atripla Avonex Avonex (interferon beta-1a) vonex Pen (interferon beta-1a) Avonex Prefilled Syringe Amersham Indium (111In) Oxine Atripla Tice BCG Vaccine (bcg) Adcetris (brentuximab) teriflunomide TheraCys (bcg) Tice BCG (bcg) Rifamate Rifater Rimactane mipomersen Rifadin Rifadin IV Kynamro (mipomersen) leflunomide lomitapide IsonaRif isoniazid / rifampin Juxtapid (lomitapide) Arava (leflunomide) Aubagio (teriflunomide) bcg
  • 27. Rheumatrex Dose Pack Sandimmune Sirturo Rebif Rebif Rebidose Revia peginterferon beta-1a Plegridy Rasuvo Otrexup Pharmorubicin PFS Pharmorubicin RDF Methotrexate LPF Sodium naltrexone Neoral indium oxyquinoline in-111 methotrexate morphine idelalisib interferon beta-1a interferon beta-1b Extavia Folex PFS Gengraf Ellence Embeda epirubicin Depade efavirenz tenofovir Clolar Contrave cyclosporine brentuximab bupropion clofarabine
  • 29.
  • 30. Ibuprofen to a class of drugs called NON-STEROIDAL ANTIINFLAMMATORY DRUGS (NSAIDS). BRANDS: Advil Medipren Motrin Nuprin Pedia care fever etc
  • 31. Ibuprofen is a non selective inhibitor of an enzyme called Cyclooxygenase (COX), which is required for the synthesis of Prostaglandins via the arachidonic acid pathway. COX is needed to convert arachidonic acid to prostaglandins H2 (PGH2) in the body. The PGH2 is then converted to prostaglandins. The inhibition of COX by ibuprofen therefore lowers the level of prostaglandins made by the body.
  • 32. Treat minor aches & pain caused by the common cold Headache Toothache Back or muscle ache Arthritis Also used to reduce fever
  • 33. Ibuprofen is contraindicated in patients with known hypersensitivity to ibuprofen. It should not be given to patients who have experienced asthma, urticaria, or allergic type reactions after taking asprin or other NSAIDS. It is contraindicated in the setting of coronary artery bypass graft (CABG) surgery. It should be avoided in pregnancy.
  • 34. Is better at reducing fever than Tylonol. Its anti- platelet properties are mild and short lived as compared to aspirin.
  • 35.
  • 37. OVERVIEW Ribavirin is antiviral agent. Ribavirin is a synthetic guanosine analogue. Ribavirin is active against several DNA and RNA viruses. Ribavirin is administered to infants and young children with respiratory syncytial virus (RSV) severe chest infections or pneumonia.
  • 38. Ribavirin also known as Tribavirin. It is of Synthetic origin and belongs to Triazoribose. t belongs to Antiviral Agents pharmacological group on the basis of mechanism of action, The Molecular Weight of Ribavirin is 244.20.
  • 39. MOA: May inhibit the initiation and elongation of RNA fragments by inhibiting polymerase activity, which in turn results in the inhibition of viral protein synthesis
  • 40. Oral absorpti on is found to be 45% . metaboli sm is reported Hepatic and Renal.
  • 43. Drug Interactions Ribavirin is known to interact with other drugs, the details of drug interactions is as follows:
  • 44. Drug Details Abacavir Didanosine Coadministration of Ribavirin and didanosine is contraindicated as because exposure to the active metabolite of didanosine are increased. Fatal hepatic failure, as well as peripheral neuropathy, pancreatitis, and symptomatic hyperlactatemia/lactic acidosis have been reported in patients receiving both didanosine and ribavirin. Interferon Alpha 2b Stavudine Ribavirin may antagonize the cell culture antiviral activity of stavudine against HIV. Zidovudine Ribavirin may antagonize the cell culture antiviral activity of Zidovudine against HIV.
  • 45.
  • 46. SIDE EFFECTS Thirst symptomaticInsomnia Headache Fatigue Metallic taste adverse Mood swings Decreas e in RBCreactions GI Disturbance
  • 47. DOSAGE Dose Single Dose Frequenc y Route Instructions Adult Dosage 400 mg 400 (400) 12 hourly PO For Hapatitis C, for 6 months. Paedriatic Dosage ( 20 Kg. ) 2.5 to 5 mg/kg 3.8 (3.75) 8 hourly Oral For 1-2 Weeks Neonatal Dosage ( 3 Kg. ) 3.125 to 6.25 mg/kg 4.7 (4.6875) 8 hourly Oral
  • 48. HIGH RISK GROUPS • Drug should not be given to Pregnant Mothers, patients suffering from Kidney dysfunction, and Neonates. WARNING / PRECAUTIONS • Ribavirin should not be used during pregnancy, since the risks outweigh the benefits. Birth control measures should be taken while using this medicine
  • 49. STORAGE CONDITIONS Inhalation Soln (freshly prepared),capsules and tablets Store at room temperature.. Protect from Sunlight and Moisture. Use within 24 hrs if kept at room temperature.
  • 50. AVAILABLE BRANDS Single Ingredient • Syrup: 50 mg, 50 mg/5ml, 100 mg/5ml • Cream: 7.5 %w/w • Tabs: 200 mg, 400 mg, 500 mg, 600 mg • Caps: 100 mg, 200 mg, 400 mg, 600 mg Multi ingredient • Syrup: 1.31 mg/5ml • Tabs: 15 mg • Copegus® • Rebetol® • Ribasphere® • Virazole®
  • 51.
  • 53. OVERVIEW It is a water-soluble hemisuccinate derivative of dihydroartemisinin. Artesunate and its active metabolite dihydroartemisinin are potent blood schizonticides, active against the ring stage of the parasite It is also active against chloroquine and mefloquine resistant strains of P. falciparum. Artesunate is ideal for the treatment of severe malaria, including cerebral malaria. It is unstable in neutral solution and is therefore only available for injections as artesunic acid.
  • 54. PRIMARY CHARACTERISTICS It is of Semi Synthetic origin. The Molecular Weight of Artesunate is 384.42. Used for oral, rectal, intravenous and intramuscular administration.
  • 55. MOA
  • 56. PHARMACOKINETICS Plasma half life is 45 min 2.4mg/kg dose in adult patients with P. falciparum malaria: Cmax: 11,330 mcg/L; Half-life: 2.7 hours; Volume of distribution: 0.14 L/kg;
  • 57. INDICATIONS Artesunate is primarily indicated in conditions like Cerebral malaria, Chloroquine resistant malaria. CONTRAINDICATIONS Artesunate is contraindicated in conditions like Hypersensitivity,Pregnancy. DRUG INTERACTIONS No data regarding the interactions of Artesunate was found.
  • 58. ADVERSE EFFECTS •lower reticulocyte counts •Flatulence, • Dizziness, • Headache, •Delayed haemolysis (occurring around two weeks after treatment) •Vomiting, • Diarrhea, •Fever, • Abdominal pain, • Rashes •Itching, • Hair loss, •Convulsions.
  • 59. AVAILABLE BRANDS Single Ingredient Inj: 60 mg, Tabs: 50 mg, Multi ingredient Tabs: 25 mg, 50 mg, 100 mg,
  • 60. DOSAGE Dose Single Dose Frequency Route Instructions Adult Dosage 2.4 mg/kg 2.4 (2.4) As recommended. IM Severe malaria: This dose is followed by 1.2mg/Kg at 12 and 24 hours then 1.2mg/Kg daily for 6 days. If the patient can swallow, the daily dose can be given orally. 2.4 mg/kg 2.4 (2.4) As recommended. IV Severe malaria: This dose is followed by 1.2mg/Kg daily until the patient can take orally artesunate or another effective antimalarial drug. 4 mg/kg 4 (4) As recommended. PO Monotherapy: 4mg/Kg loading dose on the first day followed by 2mg/Kg once a day for 6 days. 4 mg/kg 4 (4) As recommended. PO Combination therapy: 4mg/Kg once a day for 3 days plus mefloqine (15mg or 25mg of base per Kg) as a single dose or split dose on the second and/or third day.
  • 61. Paedriatic Dosage ( 20 Kg. ) No data regarding the Paedriatic dosage details of Artesunate is available. Neonatal Dosage ( 3 Kg. ) No data regarding the neonatal dosage details of Artesunate is available. INTERFERENCEIN PATHOLOGY No data regarding the pathological interferences produced by artesunate is available
  • 62.
  • 64. Amodiaquine is a 4- aminoquinoline antimalarial with an action and uses similar to that of chloroquine. Amodiaquine is not recommended for the prophylaxis of malaria. Amodiaquine is used to treat malaria
  • 65. Amodiaquine HCl is the derivative of Amodiaquine. It is of Synthetic origin and belongs to Quinoline Phenol It belongs to Antiplasmodial pharmacological group on the basis of mechanism of action and also classified in Antimalarial Agent pharmacological group.The Molecular Weight of Amodiaquine is 464.80.
  • 66. • The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function.
  • 67. • Oral absorption of Amodiaquine is found to be 82.5% ±2.5. Plasma protien binding is extensive. Presystemic metabolism is noted to be 82.5% ±2.5 and metabolism is reported via liver. Plasma half life is 5.2 hr. INDICATIONS • Amodiaquine is primarily indicated in conditions like Malaria, Nephrogenic and partial pituitary diabetes insipidus.
  • 68. • Amodiaquine is contraindicated in conditions like Malaria prophylaxis DRUG INTERACTIONS • No data regarding the interactions of Amodiaquine was found.
  • 69. • The severe or irreversible adverse effects of Amodiaquine, which give rise to further complications include Liver damage. • Amodiaquine produces potentially life-threatening effects which include Blood dyscrasias, Lupus erythematosus. which are responsible for the discontinuation of Amodiaquine therapy. • The symptomatic adverse reactions produced by Amodiaquine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Weakness, Nausea, Vomiting, Diarrhea, Abdominal cramps, Tinnitus, Irregular heart beat, Termors, General malaise, Skin pigmentation, Palate pigmentation, Nail-beds pigmentation.
  • 70. Dose Single Dose Frequency Route Instructions Adult Dosage 35 mg/kg 35 (35) As recommende d. PO For 3 days. Paedriatic Dosage ( 20 Kg. ) 5 to 10 mg/kg 7.5 (7.5) As recommende d. Oral Once a Week Neonatal Dosage ( 3 Kg. ) 6.25 mg/kg 6.2 (6.25) As recommende d. oral Once a week
  • 71. Drug should not be given to Pregnant Mothers. • WARNING / PRECAUTIONS It should be used with caution in patients allergic to peanuts, not to be used on broken, infectious skin. It should be used with caution in blockage of the gut (intestinal obstruction).
  • 72.
  • 73. Chemical class: Rifamycin. Therapeutic class: Anti tuberclosis agent,antibiotic,antinfective. Available dosage forms: It is available by mouth and intravenously.
  • 74. • Rifampicin inhibits bacterial DNA-dependent RNA synthesis by inhibiting bacterial DNA- dependent RNA polymerase.
  • 75. • Rifampicin is easily absorbed from the gastrointestinal (GI) tract. • Only about 7% of the administered drug will be excreted unchanged through the urine, About 60% to 65% is excreted through the feces. The half-life of rifampic in ranges from 1.5 to 5.0 hours. About 60% to 90% of the drug is bound to plasma proteins. Metabolized by liver. Distribution of the drug is high throughout the body, Since the substance itself is red, this high distribution is the reason for the orange-red color of the saliva, tears, sweat, urine, and feces.
  • 76. • TUBERCLOSIS. • ATYPICAL MYCOBACTERIAL INFECTIONS. • LEPROSY. • PROPHYLAXIS OF H.INFLUENZA TYPE B DISEASE IN CHILDERNS.
  • 77. Contraindicated: in jaundice and porphyria. Precautions:Liver impairment,imparts organs red colour to urine,saliva,tears,sweat and sputum,young childerns,pregnancy,breast feeding,old age.
  • 78. • GI:Anorexia,nausea,vomiting,dirrhoea. • Respiratory symptoms:SOB,collaps and shock,haemolytic anaemia,thrombocytpenia,jaundice,flushing,urtic aria,rash. • Other ADR:Edema,muscular weakness,myopathy,leucopenia,eosinophillia,me nstrual disturbances.
  • 79. • Rifampicin induce microsomal enzymes and may reduce the efficacy of following drugs: • Acetaminophin,oralanticoagulants,barbiturates,BDZ,chlor amphenicol,oral contraceptives,corticosteroids,cyclosporin,digoxin,beta blockers,slphones,theophylline,verapamil. • Halothane: Hepatotoxicity. • Isoniazid: Higher incidence of hepato toxicity than alone. • Ketokonazole: Treatment failure. • Food: Interfere with absorption of rifampicin,take on empty stomach.
  • 80. • ADULTS: • TUBERCLOSIS:450-600Mg po. • MENI NGITS:600mg bid for 2 days. • H.INFLUENZA:20Mg/kg daily for 4 days. • BRUCILLOSIS:600-1200Mg daily. • CHILDERNS: • TUBERCLOSIS:10-20Mg/kg/day po. • MENINGITIS:Under 3 months-1 year 5mg/kg bid for 2 days. • H.INFLUENZA:10Mg/kg for 4 days.
  • 81.
  • 83. Amikacin sulfate is a semi-synthetic amino glycoside antibiotic. It is used to treat different types of bacterial infections. Amikacin is most often used for treating severe, hospital-acquired infections
  • 84. • Inhibit Protein synthesis by binding directly to the 30S ribosomal subunit • causing misreading of mRNA and leaving the bacterium unable to synthesize proteins vit al to its growth.
  • 85. • Absorption: IM: May be delayed in bedridden patient • Volume of distribution: 0.25-0.4 L/kg, primarily into extracellular fluid (highly hydrophilic); penetrates blood-brain barrier when meninges inflamed; crosses placenta. • Excretion: urine (94-98%) • Half-Life: 2-3 hr Peak Plasma Time: IM: 45-120 min • Protein Binding: 0-11%
  • 86.  Central nervous system  Biliary and intestinal infection  Intraabdominal infections  Secondary infection after combustion  Infections of bones and joints. :  Patients hypersensitive to drug or other amino glycosides.  Pregnancy Breast feeding  Impaired renal function.  Neuromuscular disorders.
  • 88. Adult dose for bacteremia: Adult Dose for Pneumonia: Adult Dose for Nosocomial Pneumoni a: •15 to 22.5 mg/kg/day IV or IM in 1 to 3divided doses, •(initial maximum of 1.5 g/day, then adjust dose based on desired serum levels •5 to 22.5 mg/kg/day IV or IM in 1 to 3divided doses. •(initial maximum of 1.5 g/day, then adjust dose based on desired serum levels •20 mg/kg /day IV in 1to 3 divided doses
  • 89. • Ototoxicity • Neurotoxicity- Neuromuscular Block age • Nephrotoxicity: • Other: • skin • Rash ,headache ,nausea and vomiting, eosinophilia and hypotension
  • 90.
  • 91. Cycloserine is a second-line, broad-spectrum antibiotic, produced by Streptococcus orchidaceus. In 1955, it was first isolated from a fermentation brew and was later synthesized. Cycloserine is used in the treatment of active pulmonary and extrapulmonary tuberculosis (TB), when primary agents have failed (such as INH, rifampin, streptomycin etc). When Cycloserine is employed to treat tuberculosis, it must be given together with other effective agents. Cycloserine is given orally. It was approved by the FDA in 1956. Category: Anti- infective drugs Antibiotics, systemic Anti- tuberculosis drugs
  • 92. Cycloserine is an analog of the amino acid D-alanine. It interferes with an early step in bacterial cell wall synthesis in the cytoplasm by competitive inhibition of two enzymes, L-alanine racemase, which forms D- alanine from L-alanine, and D- alanylalanine synthetase, which incorporates D-alanine into the pentapeptide necessary for peptidoglycan formation and bacterial cell wall synthesis.
  • 93. • Used in combination with up to 5 other drugs as a treatment for Mycobacterium avium complex (MAC) and is also used to treat tuberculosis (TB) Indication • Cycloserine is contraindicated in conditions like Epilepsy, Renal failure, Hypersensitivity, Mental illness. Contraindicated
  • 94. • Oral absorption of Cycloserine is found to be 50% ±50. • Plasma protien binding is < 20%. • Presystemic metabolism is noted to be 5% ±5 and metabolism is reported hepatic. • Renal Excretion accounts for 50-70% (unchanged) and plasma half life is 10 hr. Pharmacokinetics • Congestive heart failure, Psychiatric disturbances, Megaloblastic anemia, Excitement, Convulsions, Nervous system manifestation, Vertigo, Headache, Drowsiness, Irritability, Nausea, Fever, Anxiety, Rashes, Confusion, Photosensitivity, Depression, Cardiac arrhythmias, Tremor, Disorientation, Peripheral neuropathy, Aggression, Hyper-reflexia, Confusion, Suicidal tendencies. Side Effects