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.
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
ā¢ Kidney dysfunction, Liver Malfunction, and
Neonates.
Warning / Precautions
ā¢ Minimize alcohol consumption
ā¢ Used with caution if patients have kidney or liver
problems, diabetes, history of alcohol use and of
any drug allergy.
ā¢ Avoid With Tyramine and Histamine-containing
foods e.g. fish, cheese, yeast extract or sausages.
ā¢ 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 15Ā°C-30Ā°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
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 Ā½ is approximately 1.6hr.
22. ADULTS
ā¢ PO 15 to 30 mg/kg every day or 50 to 70
mg/kg 2 times/wk.
CHILDRE
N
ā¢ PO 15 to 30 mg/kg every day or 50 to 70
mg/kg 2 times/wk
ADMINIST
R
ATION
ā¢ Administer without regard to meals.Administer
with food if GI upset occurs.
STORAG
E/STABLI
TY
ā¢ Store at room temperature (59Ā° to 86Ā°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.
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.
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
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.
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
ā¢ Drug should not be given to Pregnant
Mothers, patients suffering from
Kidney dysfunction, and Neonates.
WARNING / PRECAUTIONS
ā¢ 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.
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.
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.
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
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. ā¢ 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. ā¢ Oral absorption of Amodiaquine is found to
be 82.5% Ā±2.5. Plasma protien binding is
extensive. Presystemic metabolism is noted
to be 82.5% Ā±2.5 and metabolism is reported
via liver. Plasma half life is 5.2 hr.
INDICATIONS
ā¢ Amodiaquine is primarily indicated in
conditions like Malaria, Nephrogenic and
partial pituitary diabetes insipidus.
68. ā¢ Amodiaquine is
contraindicated in
conditions
like Malaria
prophylaxis
DRUG
INTERACTIONS
ā¢ No data regarding
the interactions of
Amodiaquine was
found.
69. ā¢ The severe or irreversible
adverse effects of
Amodiaquine, which give
rise to further
complications include
Liver damage.
ā¢ Amodiaquine produces
potentially life-threatening
effects which include
Blood dyscrasias, Lupus
erythematosus. which are
responsible for the
discontinuation of
Amodiaquine therapy.
ā¢ 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.
ā¢ 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.
75. ā¢ Rifampicin is easily absorbed from
the gastrointestinal (GI) tract.
ā¢ 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. ā¢ TUBERCLOSIS.
ā¢ ATYPICAL MYCOBACTERIAL INFECTIONS.
ā¢ LEPROSY.
ā¢ 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. ā¢ GI:Anorexia,nausea,vomiting,dirrhoea.
ā¢ Respiratory symptoms:SOB,collaps and
shock,haemolytic
anaemia,thrombocytpenia,jaundice,flushing,urtic
aria,rash.
ā¢ Other ADR:Edema,muscular
weakness,myopathy,leucopenia,eosinophillia,me
nstrual disturbances.
79. ā¢ Rifampicin induce microsomal enzymes and may reduce
the efficacy of following drugs:
ā¢ Acetaminophin,oralanticoagulants,barbiturates,BDZ,chlor
amphenicol,oral
contraceptives,corticosteroids,cyclosporin,digoxin,beta
blockers,slphones,theophylline,verapamil.
ā¢ Halothane: Hepatotoxicity.
ā¢ Isoniazid: Higher incidence of hepato toxicity than alone.
ā¢ Ketokonazole: Treatment failure.
ā¢ Food: Interfere with absorption of rifampicin,take on
empty stomach.
80. ā¢ ADULTS:
ā¢ TUBERCLOSIS:450-600Mg po.
ā¢ MENI NGITS:600mg bid for 2 days.
ā¢ H.INFLUENZA:20Mg/kg daily for 4 days.
ā¢ BRUCILLOSIS:600-1200Mg daily.
ā¢ CHILDERNS:
ā¢ TUBERCLOSIS:10-20Mg/kg/day po.
ā¢ MENINGITIS:Under 3 months-1 year 5mg/kg bid for 2
days.
ā¢ H.INFLUENZA:10Mg/kg for 4 days.
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. ā¢ Inhibit Protein
synthesis by binding
directly to the
30S ribosomal subunit
ā¢ causing misreading
of mRNA and leaving
the bacterium unable
to
synthesize proteins vit
al to its growth.
85. ā¢ Absorption: IM: May be delayed in
bedridden patient
ā¢ Volume of distribution: 0.25-0.4 L/kg,
primarily into extracellular fluid (highly
hydrophilic); penetrates blood-brain barrier
when meninges inflamed; crosses
placenta.
ā¢ Excretion: urine (94-98%)
ā¢ Half-Life: 2-3 hr Peak Plasma Time: IM:
45-120 min
ā¢ Protein Binding: 0-11%
86. ļ± Central nervous
system
ļ± Biliary and intestinal
infection
ļ± Intraabdominal
infections
ļ± Secondary infection
after combustion
ļ± Infections of bones
and joints.
:
ļ± Patients
hypersensitive to drug
or other amino
glycosides.
ļ± Pregnancy
ļ±Breast feeding
ļ± Impaired renal
function.
ļ± Neuromuscular
disorders.
88. Adult dose for
bacteremia:
Adult Dose
for Pneumonia:
Adult Dose
for Nosocomial Pneumoni
a:
ā¢15 to 22.5 mg/kg/day
IV or IM in 1 to 3divided
doses,
ā¢(initial maximum of 1.5
g/day, then adjust dose
based on desired serum
levels
ā¢5 to 22.5
mg/kg/day IV or IM in 1
to 3divided doses.
ā¢(initial maximum of 1.5
g/day, then adjust dose
based on desired serum
levels
ā¢20 mg/kg /day IV
in 1to 3 divided doses
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. ā¢ 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
ā¢ Cycloserine is contraindicated
in conditions like Epilepsy,
Renal failure, Hypersensitivity,
Mental illness.
Contraindicated
94. ā¢ Oral absorption of Cycloserine is found to be 50%
Ā±50.
ā¢ Plasma protien binding is < 20%.
ā¢ Presystemic metabolism is noted to be 5% Ā±5 and
metabolism is reported hepatic.
ā¢ Renal Excretion accounts for 50-70% (unchanged)
and plasma half life is 10 hr.
Pharmacokinetics
ā¢ 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