Drug Profile A practical approach to give basic knowledge about the drugs pharmacy

Prepare Drug Profile of Aspirin

Active ingredient: Aspirin (Acetylsalicylic Acid)

Drug Category (PRESCRIPTION/OTC): OTC and prescription both

WHO Essential Drug List: It is on the WHO essential drug list

1. PRODUCT DESCRIPTION
Sr. Brand Manufacturer Dosage Strength Price/unit
No. Name Form
ASPIRIN Wilshire Tablets 300mg Rs.150
1 laboratories (pvt)
ltd
2 EROCID Eros Tablets 300mg Rs.150
pharmaceuticals

3 SOLUPRIN Lisko Pakistan Tablets 300mg Rs.55

(pvt) ltd

4 ASPIRIN Medicaids Tablets 300mg Rs.106.96

Pakistan (pvt) ltd

5 ANTICLOT Euro pharma Tablet 75mg Rs.26

international

How to store this drug:

 Aspirin can be administered through oral, rectal, and intravenous (IV) route
 Tablet: Store in a well closed container, Below 40°C. Protect from Sunlight and
Moisture.
 SUPPOSITORIES: Store in a well closed container. Refrigeration is recommended.
Do not Freeze. Protect from Sunlight and Moisture.
 Keep out of the reach of children.

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 Drug Profile A practical approach to give basic knowledge about the drugs pharmacy

2. CHEMISTRY OF DRUG:
Chemical Class:
Benzene and substituted derivatives

Chemical Nature/Structure:

Physical Properties:
Aspirin, an acetyl derivative of salicylic acid, is a white, crystalline, weakly acidic
substance, with a melting point of 136 °C (277 °F), and a boiling point of 140 °C (284
°F).

3. PHARMACOKINETICS:
i) ABSORPTION:
Aspirin rapidly absorbed from the gastrointestinal tract when administered as a
solution,slow absorption with tablets. Oral absorption of Aspirin is found to be 85%
±5.
ii) DISTRIBUTION:

Bio- Protein Placental Blood Secreted Volume of Time

avail- Binding Barrier Brain in Distribution for
ability (%) Barrier Milk Onset
of
Action
50%(oral) 50% to 90% It is known yes yes 0.1–0.2 L/kg. 5-30 min
to cross the
placenta. 

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 Drug Profile A practical approach to give basic knowledge about the drugs pharmacy

iii) ELIMINATION
Half Life Site of Metabolism Active Metabolite Route of
(if Any) Excretion
Dose dependent Liver (CYP2C19 and salicylic acid, Urine (80-100%), sweat,
2-3hrs (low dose) possibly CYP3A), salicyluric acid, the saliva, feces
15h-30h (large dose) some is also ether or phenolic
hydrolysed to glucuronide and the
salicylate in the gut ester or acyl
wall glucuronide. A small
portion is converted to
gentisic acid and
other hydroxybenzoic
acids 

4. CLINICAL PHARMACOLOGY:

Pharmacological
 Salicylate
class

Therapeutic Class nonnarcotic analgesic, antipyretic, anti-inflammatory, antiplatelet

Mechanism of Acetylsalicylic acid (ASA) blocks prostaglandin synthesis. It is non-

action selective for COX-1 and COX-2 enzymes Inhibition of COX-1 results
in the inhibition of platelet aggregation for about 7-10 days (average
platelet lifespan). The acetyl group of acetylsalicylic acid binds with
a serine residue of the cyclooxygenase-1 (COX-1) enzyme, leading to
irreversible inhibition. This prevents the production of pain-causing
prostaglandins. This process also stops the conversion of
arachidonic acid to thromboxane A2 (TXA2), which is a potent
inducer of platelet aggregation
Spectrum (in
case of
antibiotic)
Hypersensitivity, bleeding disorders such as hemophilia, von
Contraindications Willebrand’s disease, or telangiectasia, in patients with NSAID-
induced sensitivity reactions and in children with chickenpox or
flulike symptoms, Hypoprothrombinemia

  Usecautiously in patients with GI lesions, impaired renal function,

Precautions vitamin K deficiency, thrombotic thrombocytopenic purpura, or
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 Drug Profile A practical approach to give basic knowledge about the drugs pharmacy

hepatic impairment. severe anemia, and patients intolerant to

salicylate

FDA pregnancy category D

class

Clinically Monitoring Parameters

 Monitor vital signs frequently, especially temperature.
 Carefully evaluate patients at risk for infections, such as those with diabetes.
 Monitor CBC, platelets, PT, BUN, serum creatinine, and liver function studies
periodically during salicylate therapy to detect abnormalities.
 Assess patient for signs and symptoms of hemorrhage, such as petechiae, bruising,
coffee ground vomitus, and black tarry stools.

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 5. DOSAGE SCHEDULE
Sr. Recommended Dosage Duration
No. Route of
Indication Administration of therapy
Child Adult (if any)
1 Osteoarthritis Oral 60-130 mg/kg 3g/day in
daily in divided doses -
divided
doses.
2 Fever Oral >12years: 300-600mg
300-650mg q4-6hr
q4-6hrs Max dose: 4g -
Max dose: 4g in 24 hrs
in 24 hrs
3 Myocardial Oral Initial:160- 30 days
infarction 162.5mg
Maintenance:
- 160-162.5mg
OD for 30
days (post
infarction)
4 Angina pectoris Oral Immediate
prophylaxis release:75-
325mg OD
- Extended -
release:162m
g OD
5 Ischemic stroke Oral Immediate
release: 50-
325mg OD
- Extended -
release:
162.5mg OD
6 Kawasaki Oral Initial: 80- Initial: 80- 6 to 8 weeks
(mucocutaneous 100 mg/kg in 100 mg/kg
lymph node) divided doses daily in four
syndrome. divided
doses.
 6. ADJUSTMENT OF DOSAGE (if required) IN RENAL/HEPATIC
IMPAIRMENT:
Renal impairment:
 CrCl less than 10 mL/min: Contraindicated
 CrCl 10 mL/min or greater: Use with caution
Hepatic impairment:
 Severe hepatic impairment: Contraindicated
 Mild to Moderate hepatic impairment: Use with caution
7. SIDE EFFECTS:
Common: dyspepsia, epigastric discomfort, heartburn, and nausea, Dizziness, Vertigo,
Nausea, Vomiting, Tinnitus, Epigastric discomfort, , Asthma, Respiratory alkalosis, Bleeding,
loss of appetite
Severe: Cerebral hemorrhage, Airway obstruction, Gastric ulceration, Gastric erosion,
Renal failure, Hyperkalemia, Cardiovascular collapse, 

8. ADMINISTRATION GUIDELINES:
How to take this drug: take the medicine with full, glass of water

Can you break or crush tablets: Tablets may be chewed, broken, or crumbled and
administered with food or fluids to aid swallowing.
Counseling about the drug:
 Advise patient to sit up for 15 to 30 minutes after taking salicylates to prevent lodging
of salicylate in esophagus.
 Uncoated plain aspirin tablets allowed to remain in contact with mucous membranes of
the mouth and aspirin-containing chewing gum have produced mucosal erosions and
mouth ulcerations.
 Moisture may cause aspirin to lose potency. Store in a cool, dry place, and avoid using
if tablets smell like vinegar.
 Tell patient to take drug with food or after meals to avoid GI upset.
 An allergic reaction occurs. Seek medical help right away.

INSTRUCTION FOR TOPICAL USE (IF ANY):

 Aspirin is being used for a number of topical indications like Erythromelalgia (burning
sensation and redness over the extremities), Vitiligo(acquired idiopathic pigmentary
disorder) etc.
 Apply the medication to the affected area no more than 3 to 4 times a day. Rub in
 gently and thoroughly. After applying the medication, wash your hands unless you are
using this medication to treat the hands.
 Do not apply this medication on broken or irritated skin. Do not bandage or tightly
wrap the affected area or apply heat to the area (such as using a heating pad).

FOR I/V ROUTE

Solvent For Reconstitution
water for injection
(for dry powder for injection)

5ml
Volume To Be Added/
Concentration
Store below 25
Temperature And Storage
Time After Reconstitution
Glucose 5%, sodium chloride 0.9%
Compatible IV fluids
 9. DRUG-DRUG/FOODINTERACTIONS
Interacting Severity Mechanism Outcome Management
Drug
Ibuprofen Major Ibuprofen Gastrointestinal -Avoid the regular use of
competitively inhibit (GI) toxicity, ibuprofen and possibly other
platelet cyclogenase including nsaids
and cause temporary inflammation, -Occasional use of ibuprofen
depression on bleeding, is acceptable
thromboxane ulceration, and -For necessary concomitant
formation thereby perforation. use diclofenac may be viable
antagonize aspirin’s alternative
function
Methotrexate Major Aspirin can interfere Increased Avoid concomitant use
with  the renal pharmacological otherwise monitor the
elimination of effect of patient for signs of bone
methotrexate and may methotrexate marrow depression or other
displace it from leading to toxicity side effects
binding sites. symptoms of
which include
nausea, vomiting,
diarrhea,
stomatitis, sore
throat, chills,
fever, rash etc.
Warfarin Major Major aspirin Prolonged -Their combined use should
alongwith warfarin bleeding time, generally be avoided
additively inhibits gastrointestinal -If concomitant therapy is
platelet aggregation lesions, unusual used for additive
and add upto its bruising, anticoagulant effects,
anticoagulant effect vomiting, blood monitoring for excessive
in your urine or anticoagulation and overt
stools, headache, and occult bleeding is
dizziness, or recommended
weakness
Diclofenac Moderate Aspirin displace gastrointestinal Concomitant administration
NSAIDs from plasma (GI) toxicity, is considered
protein binding sites including contraindicated.
resulting in increased inflammation,
concentration of bleeding,
unbound, or free, ulceration, and
drug available for perforation
clearance
Ethanol Moderate Concurrent use GI blood loss Patient should be advised to
additively inhibit refrain from alcohol
prostaglandins consumption while taking
leading to decreased aspirin
integrity of the GI
lining
Garlic Moderate Garlic additively Increased risk of Avoid large amount of garlic
potentiates aspirins bleeding or garlic supplements during
anticoagulant and (prolonged use of aspirin.
antithrombotic bleeding from
effects. cuts, increased
menstrual flow,
vaginal bleeding,
nosebleeds,
bleeding of gums
from brushing,
unusual bleeding)
Ginkgo Moderate Ginkgo also inhibits Increased Avoid their combined use
platelet aggregation bleeding with risk Discontinue the use of ginkgo
atleast 2 weeks prior to surgery
by inhibiting platelet of developing
activating factor and hemorrhage
adds to aspirins
anticoagulant effect
 Toxic Dose Signs & Symptoms of Management/Treatment
Toxicity (including antidote)
>300mcg/L or Mild toxicity: tinnitus, dizziness, -Alkalization of the urine can be
therapeutic doses to as lethargy, nausea, and vomiting achieved via a bicarbonate drip
high as 70-140 mg/dL severe toxicity: hyperthermia, (3 ampules of 50 meq/50 ml for
accounts for acute tachypnea leading to respiratory a total of 150 meq in 1000 ml of
toxicity alkalosis, high anion gap D5W)
metabolic acidosis, hypokalemia, -Doctors may use gastric
hypoglycemia, seizures, coma lavage, or pumping out
and cerebral edema. the stomach contents, to try to
prevent further absorption of
the aspirin into the
body. Dialysis is also
sometimes used to reduce the
amount of salicylate in the body
-To prevent more absorption,
the doctor may give activated
charcoal to absorb the
salicylate from the stomach. A
laxative may be given with the
activated charcoal to move the
mixture through the
gastrointestinal system more
rapidly. People who have been
severely poisoned may be given
repeated doses of activated
charcoal.

10. TOXICOLOGY