MORPHINE (Generic)

Drug Profile

2. Brand(s):

Brand Name	Manufacturer	Dosage Form	Pack Size	MRP
Morphine sulphate		Injection

3. Pharmacological Group:

                                                      Narcotic pain relievers.

4. Formulation:

                                 Ampoule (0.5-50mg/ml of morphine)

5. General Information:

 Morphine is a highly addictive substance, both psychologically and physically.   tolerance, physical and psychological dependences develop very rapidly:

6. Dosage Form:

Solids

Tablets

Capsules
Hard Capsules	Soft Capsules	Modified Released Capsules

Uncoated Tablets

Coated Tablets

Modified Released Tablets

Sublingual Tablets

Powders
Powders for suspension	Powders for Inhalers

Others

Liquids

Syrup

Oral drops

Nasal Drops

Topical Solutions

Eye Preparations

Ear Preparations

Others

Parenterals Preparations ◘

Injection

Infusions

Powders for injection

Others

Topical Solids

Ointment

Creams

lotions

Gels

Pastes

Others

6. Therapeutic Uses:
 Morphine is used legally:

• as an analgesic in hospital settings to relieve
• pain in myocardial infarction
• pain in sickle cell crisis
• pain associated with surgical conditions, pre- and postoperatively
• pain associated with trauma
• in the relief of severe chronic pain, e.g.,
• cancer
• pain from kidney stones (renal colic, ureterolithiasis)
• severe back pain
• as an adjunct to general anesthesia
• in epidural anesthesia or intrathecal analgesia
• as an antitussive for severe cough

7. Information for the user:

i. How to take:

Use this medication exactly as it was prescribed for you. Never take morphine in larger amounts, or use it for longer than recommended by your doctor. Follow the directions on your prescription label

ii. Frequency & Time of Doses:

                                                      8-20 mg IM bd

iii. Recommended Dosage Range:

Neonates/ Children	Adult	Geriatric	Dose according to clinical condition
Oral 0.3 mg/kg q 3-4 hrs Parenterals 0.1mg/kg q 3-4 hrs	Oral 30mg q 3-4 hrs Parentrals 10mg 3-4 hrs

iv. Onset of effect:

                                 60 min

v. duration of action

                               60-90 min

vi. Diet Advice:

                           Drink plenty of fluids while you are taking this medication

vii. Storage:

Store this medication at room temperature, away from heat, moisture, and light. Keep track of how many pills have been used from each new bottle of this medicine. .After you have stopped using this medication, flush any unused pills down the toilet. Throw away any unused liquid morphine that is older than 90 days.

viii: Missed Dose:

Since morphine is sometimes used as needed, you may not be on a dosing schedule. If you are using the medication regularly, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and wait until your next regularly scheduled dose. Do not use extra medicine to make up the missed dose.

ix. Stopping the drug:

Do not stop using morphine suddenly, or you could have unpleasant withdrawal symptoms. Talk to your doctor about how to avoid withdrawal symptoms when stopping the medication.

x. Exceeding the dose (overdose):

Seek emergency medical attention if you think you have used too much of this medicine. An overdose of morphine can be fatal. Overdose symptoms may include extreme drowsiness, pinpoint pupils, confusion, cold and clammy skin, weak pulse, shallow breathing, fainting, or breathing that stops.

8. Possible Adverse Effects:

·         shallow breathing, slow heartbeat;

·         seizure (convulsions);

·         cold, clammy skin;

·         confusion;

·         severe weakness or dizziness; or

• feeling light-headed, fainting.
• upset stomach
• vomiting
• constipation
• stomach pain
• rash
• difficulty urinating

9. Contraindications:

Hypersensitivity to morphine

Respiratory and CNS depression with respiratory failure

Suspected head injury it may cause exaggerated CNS depression

10. Interactions:

Drug-Drug Interactions	Drug-Food Interactions
MAO inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil) other narcotic pain medications, sedatives, tranquilizers, muscle relaxers, or other medicines that can make you sleepy or slow your breathing.	Check your food and medicine labels to be sure these products do not contain alcohol

11. Prolonged Use:

                                      Results in the addiction

12. Special Precautions:

 i. Be sure to tell your doctor if:

if you are using pentazocine (Talwin), nalbuphine (Nubain), butorphanol (Stadol), or buprenorphine (Buprenex, Subutex). If you are using any of these drugs, you may not be able to use morphine, or you may need dosage adjustments or special tests during treatment. if you have ever had an allergic reaction to a narcotic medicine (examples include codeine, methado),asthma attack a history of head injury or brain tumor;  epilepsy or other seizure disorder; low blood pressure; gallbladder disease; Addison's disease or other adrenal gland disorders; enlarged prostate, urination problems; a history of drug or alcohol addiction

ii. Pregnancy:

                        Morphine diffuses across the placenta

iii. Breast Feeding/Lactation:

Traces appear in breast milk It may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

iv. Infants & Children:

                                       Same pharmacological effect as in adult

v. Over 60:

Older adults may be more sensitive to the effects of this medicine.

vi. Driving & Hazardous work:

                                                       Impair thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

 vii. Alcohol:

                       Do not drink alcohol while you are taking this medication. Dangerous side effects or death can occur when alcohol is combined with morphine

13. Pharmacological Properties:

13.(i). Pharmacodynamic Properties:

It binds to specific .G protein –coupled receptor ,located primarily in brain and spinal cord regions involved in the transmission  and modulation of pain.

13.(ii). Pharmacokinetic Properties:

i. Absorption:

                         Well absorbed in GIT

ii. Distribution:

Bioavailability	%Protein binding	Half Life	Volume of distribution	Blood Brain Barrier	Placental Barrier
Oral 25% I M 100%	35%	2-3 hrs	3.3 L/kg	poorly	crosses

iii. Metabolism

Site of Metabolism	Active Metabolites
Liver and Gut	Morphine-3-glucuronide, Morphine-6-glcrounide,nor morphine, codiene

iv. Elimination:

Elimination Half Life	Route of Elimination
1.7 hrs	10% through feaces 90% through urine

15. Preclinical Safety Data:

                                                      In biphasic cortisole response also has been observed for narcotics. Morphine administered to rats is known to block the release of cortisole in response to histamine challenge by inhibiting release of ACTH.s

16. Instructions for Handling:

Keep track of how many pills have been used from each new bottle of this medicine. Morphine is a drug of abuse and you should be aware if any person in the household is using this medicine improperly or without a prescription.

INDOMETACIN (Generic)

Drug Profile

2. Brand(s):

Brand name	Manufactruer	Dosage form	Pack Size	MRP
Indobid	Adamjee	Capsule	50*10	Rs 251.68
Indocap	Hamaz	Capsule	1000	Rs 217.60
Indacin	KPL	Capsule	1000	Rs 284.68
Epomet	Epoch	Capsule	50*10	Rs 343.74

3. Pharmacological Group:

                                            NON-STEROIDAL ANTI-INFLAMMATORY DRUG

4. Formulation:

                                     Capsules containing 25mg Indomethacin

5.  General Information:

                                                   Indomethacin is a non-steroidal anti-inflammatory drug commonly used to reduce fever, pain, stiffness, and swelling. It works by inhibiting the production of prostaglandins, molecules known to cause these symptoms

.6. Dosage Form:

Solids

Tablets

Capsules
Hard Capsules    ◙	Soft Capsules	Modified Released Capsules

Uncoated Tablets

Coated Tablets

Modified Released Tablets

Sublingual Tablets

Powders
Powders for suspension	Powders for Inhalers

Others

Liquids

Syrup

Oral drops

Nasal Drops

Topical Solutions

Eye Preparations

Ear Preparations

Others

Parenterals Preparations

Injections

Infusions

Powders for injection

Others

Topical Solids

Ointment

Creams

lotions

Gels

Pastes

Others

6. Therapeutic Uses:

Renal colic (pain due to kidney stones), cryoglobulinemia, bartter syndrome, dysmenorrhea (menstrual cramps), pericarditisnephrogenic, diabetes insipidus (prostaglandin inhibits vasopressin's action in the kidney), fever and pain associated with malignant diseases (tumors, bony metastases, lymphogranulomatosis, rheumatoid arthritis, arthritic gout, osteoarthritis

7. Information for the user:

i. How to take:

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.Take indomethacin with food or milk to lessen stomach upset. Do not crush, chew, break, or open an extended-release capsule.

ii. Frequency & Time of Doses

                                                     2 to 3 times a day

iii. Recommended Dosage Range:

Neonates/ Children	Adult	Geriatric	Dose according to clinical condition
Orally 200µg/kg bd	200mg tid

iv. Onset of effect:

                                      30 min

v. Duration of Action:

                                      4-6 hrs

vi. Diet Advice:

                          Unless your doctor tells you otherwise, continue your normal diet

vii. Storage:

                    Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture

viii: Missed Dose:

If you are taking indomethacin on a regular schedule, take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose.

If you are taking indomethacin as needed, take the missed dose if it is needed, then wait the recommended or prescribed amount of time before

ix. Stopping the drug:

                                     Stopping the Drug at once after the completion of therapy may not produce any harmful  symptoms but a low dose regime is required to avoid relapse.

x. Exceeding the dose (overdose):

Seek emergency medical attention if you think you have used too much of this medicine. Symptoms of an indomethacin overdose may include nausea

8. Possible Adverse Effects:

Chest pain, weakness, shortness of breath, slurred speech, problems with vision or balance; black, bloody, or tarry stools coughing up blood or vomit that looks like coffee grounds dizziness, nervousness, headache;

9. Contraindications

• concurrent peptic ulcer, or history of ulcer disease
• allergy to indomethacin, aspirin, or other NSAIDs
• patients with nasal polyps reacting with an angioedema to other NSAIDs
• children under 2 years of age (with the exception of neonates with patent ductus arteriosus)
• severe pre-existing renal and liver damage
• caution: pre-existing bone marrow damage (frequent blood cell counts are indicated)
• caution: bleeding tendencies of unknown origin (indomethacin inhibits platelet aggregation)
• caution: Parkinson's disease, epilepsy, psychotic disorders (indomethacin may worsen these conditions)

10. Interactions:

Drug-Drug Interactions	Drug-Food Interactions
Aspirin or other NSAIDs warfarin (Coumadin); cyclosporine Digoxin diuretics such as furosemide Methotrexate steroids a beta-blocker such as atenolol.	Using alcohol or tobacco with Indomethacin may cause interactions to occur. Vit C rich food can leads to Kidney stones.

11. Prolonged Use:

Patients should undergo regular physical examination to detect edema and signs of central nervous side effects. Blood pressure checks will reveal development of hypertension. Periodic serum electrolyte (sodium, potassium, chloride) measurements, complete blood cell counts and assessment of liver enzymes as well as of creatinine (renal function) should be performed. This is particularly important if indomethacin is given together with an ACE inhibitor or with potassium-sparing diuretics, because these combinations can lead to hyperkalemia and/or serious kidney failure. No examinations are necessary if only the topical preparations (spray or gel) are applied.

12. Special Precautions:

 i. Be sure to tell your doctor if:

If you are allergic to indomethacin, aspirin or other NSAID

If you have or have ever had asthma, especially if you also have frequent stuffed or runny nose or nasal polyps (swelling of the lining of the nose); seizures; Parkinson's disease; depression or mental illness; or liver or kidney disease. If you will be using indomethacin suppositories, also tell your doctor if you have or have ever had proctitis (inflammation of the rectum) or have or have recently had rectal bleeding.

ii. Pregnancy:

 Not save because in pregnancy it adversely effect the fetus

iii. Breast Feeding/Lactation:

Appears in breast milk and cause convulsion in 1 week old infant.

iv. Infants & Children:

                                       Use with precaution in infants

v. Over 60:

                    Maintenance dose should be reduced by 25% b/c total clearance is reduced as compared to young subject

vi. Driving & Hazardous work:

                                                          Do not drive a car or operate machinery.

vii. Alcohol:

                       Alcohol can add to the drowsiness caused by this medication.

13. Pharmacological Properties:

13.(i). Pharmacodynamic Properties:

Indomethacin is a nonselective inhibitor of cyclooxygenase (COX) 1 and 2, enzymes that participate in prostaglandin synthesis from arachidonic acid. Prostaglandins are hormone-like molecules normally found in the body, where they have a wide variety of effects, some of which lead to pain, fever, and inflammation.

13.(ii). Pharmacokinetic Properties:

i. Absorption:

                        Rapidly and completely absorbed from GIT after oral administration.

ii. Distribution:

Bioavailability	%Protein binding	Half Life	Volume of distribution	Blood Brain Barrier	Placental Barrier
~100% (oral), 80–90% (rectal)	99%	4.5 hours	0.3-0.9 L/kg		crosses

iii. Metabolism

Site of Metabolism	Active Metabolites
Hepatic	0 demethylation conjugated with glucronic acid 10% N-deacylation

iv. Elimination:

Elimination Half Life	Route of Elimination
4 to 5 hrs	Renal 60%, faecal 33%

15. Preclinical Safety Data:

Indomethacin has a high acute toxicity both for animals (12 mg/kg in rats and 50 mg/kg in mice) and for humans. Exact human data does not exist, but some fatal human cases, particularly in children and adolescents, have been seen.

16. Instructions for Handling:

Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.