Erythromycin (Oral): Uses, Dosage, Side Effects

Generic Name

Erythromycin (Oral)

Therapeutic Class: Anti-diarrhoeal antimicrobial drugs, Macrolides

Indications

Erythromycin is highly effective in the treatment of a wide variety of clinical infections.
Upper respiratory tract infections: Tonsilitis, Peritonsillar abscess, Pharyngitis, laryngitis, Sinusitis. Secondary infections in colds and influenza.
Lower respiratory tract infections: Tracheitis, acute and chronic bronchitis.
Ear infections: Otitis media, otitis externa, mastoiditis.
Eye infections: Blepharitis, established trachoma.
Skin and Soft tissue infections: Boils and carbuncles, impetigo, abscesses, pustular acne, paromychia, cellulitis, erysipelas.
Gastrointestinal tract infections: Cholecystitis, staphylococcal enterocolitis.
Prophylaxis: Pre and post-operative, trauma, burns, rheumatic fever.
Other infections: Osteomyelitis, diptheria, scarlet fever, whooping cough.

Description
Erythromycin belongs to the macrolides group of antibiotics. It exerts a bacteriostatic or bactericidal action based on specific interference with ribosomal protein synthesis within the bacterial cell. THROCIN is mainly used for the treatment of infections caused by penicillinase producing staphylococci.

The following micro-organisms are particularly susceptible to Erythromycin. Gram (+)ve : Cocci and bacilli. Gram (-)ve : Neisseria catarhalis, N.meningitis, N.gonorrhoea, Haemophilus influenzae, Brodetella, H. pertussis.Other micro-organisms : Mycoplasma pneumoniae, Legionella pneumophila, Bacteroides fragilis, B.oralis, B.melaninogenicus, Fusobacterium, Chlamydia trachomatis, Treponema pallidum.

Pharmacology
Erythromycin inhibits microsomal protein synthesis in susceptible organisms by inhibiting the translocation process. Specific binding to the 50S subunit or 70S ribosome occurs in these organisms but there is no binding to the stable 80S mammalian ribosome. Erythromycin is active against many Grampositive bacteria, some Gram-negative bacteria and against mycoplasmas and chlamydia.

Absorption: Erythromycin base is destroyed by acid and is therefore administered in the form of stable ester. The rates of absorption of the base and esters are diminished by the presence of food. The stearate is hydrolyzed in the intestine and the free erythromycin absorbed.

Blood concentration: After an oral dose of 500 mg. of the base of stearate, peak serum concentrations of 0.9 to 1.4 or 0.4 to 1.8 mg/ml. respectively are attained in 1 to 4 hours. Half-life: The serum half-life is 1.2 to 4 hours. In subjects with oliguria, the half-life is about 5 hours.

Distribution: Erythromycin is widely distributed throughout body tissue and fluids with some retention in the liver and spleen, protein binding of erythromycin base is 73%. Erythromycin enters the cerebrospinal fluid when the meninges are inflamed. It also crosses the placenta and is excreted in the milk.

Excretion: 5 to 15 % of the dose of erythromycin is excreted in the urine and large amounts of the unchanged active substance are excreted in the bile.

Dosage & Administration

Adult and Children over 8 years: 250-500 mg every six hours for mild to moderate infections. This may be increased upto 4 gm. or more daily in severe cases.
Elderly: No special dosage recommendation. Erythromycin may be administered if desired, three times daily or twice daily by giving one-third or half of the total daily requirement 8 hourly or 12 hourly respectively.
Children aged 2 to 8 years: 250 mg. every six hours or 30-50 mg/kg body weight per day divided into four equal dosage.
Infants and Children upto 2 years: 500 mg. in divided doses or 30-50 mg/kg body weight in divided doses.

Interaction
Recent data from studies of erythromycin reveals that its use in patients who are receiving high dosage of theophylline may be associated with an increase of serum theophylline levels and potential theophylline toxicity. In such cases this dose of theophylline should be reduced.

Contraindications
Known hypersensitivity to Erythromycin.

Side Effects
Allergic reactions are rare and mild although anaphylaxis has occurred. Occasionally there is abdominal discomfort after oral administration, sometimes with nausea and vomiting. This discomfort usually subsides after a few days without it being necessary to reduce the dosage.

Pregnancy & Lactation
Clinical and Laboratory studies have been shown no evidence in human of teratogenicity or toxicity. However, caution should be exercised when prescribing this drug to pregnant patients and lactating mothers since erythromycin crosses the placental barrier and is excreted in breast milk.

Precautions & Warnings
Erythromycin should be given with care in patients with impaired hepatic function, as erythromycin is excreted principally in the bile.

Overdose Effects
In case of overdosage, Erythromycin should be discontinued. Overdosage should be handled with the prompt elimination of unabsorbed drug and all other appropriate measures should be instituted. Erythromycin is not removed by peritoneal dialysis or haemodialysis.

Reconstitution
Direction for reconstitution of suspension: Shake the bottle to loosen powder. Add 60 ml or 100 ml of boiled and cooled water to the dry powder of the bottle. For ease of preparation, add water to the bottle in two proportions. Shake well after each addition until all the powder is in suspension.

Shake the suspension well before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in refrigerator and unused portion should be discarded after 7 days.

Storage
Keep below 25°C temperature, away from light & moisture. Keep out of the reach of children.

Eperisone Hydrochloride: Uses, Dosage, Side Effects

Generic Name

Eperisone Hydrochloride

Therapeutic Class: Centrally acting Skeletal Muscle Relaxants

Indications
Improvement of muscular hypertonic symptoms in the following diseases: cervical syndrome, periarthritis of the shoulder, lumbago. Spastic paralysis in the following disease: Cerebrovascular disease, spastic spinal paralysis, cervical spondylosis, postoperative sequelae (including cerebrospinal tumor), sequelae to trauma (spinal trauma, head injury), amyotrophic lateral sclerosis, cerebral palsy, spinocerebellar degeneration, spinal vascular diseases and other encephalomyelopathies.

Pharmacology
Eperisone is centrally acting skeletal muscle relaxant used to improve myotonic symptoms.

Dosage & Administration
For adults: Usually 3 tablets per day in three divided doses after each meal. The dosage should be adjusted depending on the patient age and severity of symptoms.

Interaction
Avoid concomitant use with tolperisone HCl and methocarbamol.

Contraindications
Eperisone is contraindicated in patients with a history of hypersensitivity to Eperisone Hydrochloride.

Side Effects
The side effects of Eperisone are very rare, only a few cases have been observed. These are excessive relaxation, stomachache, nausea, vertigo, anorexia, drowsiness, skin rashes, diarrhea, vomiting, indigestion, GI disturbances, insomnia, headache, constipation, etc.

Pregnancy & Lactation
Eperisone should only be used in pregnant women if the expected therapeutic benefits are evaluated to outweight the possible risks of treatment. The safety of Eperisone has not been established in pregnant women. The drug should not be used during lactation.

Storage
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.

Entecavir: Uses, Dosage, Side Effects

Generic Name

Entecavir

Therapeutic Class: Hepatic viral infections (Hepatitis B)

Indications
Entecavir is indicated for the treatment of chronic hepatitis B virus infection in adults and pediatric patients 2 years of age and older with evidence of active viral replication and either evidence of persistent elevation in serum aminotransferases (ALT or AST) or histologically active disease.

Pharmacology
By competing with the natural substrate deoxyguanosine triphosphate, entecavir functionally inhibits all three activities of the HBV polymerase (reverse transcriptase, rt):
Base priming,
Reverse transcription of the negative strand from the pregenomic messenger RNA, and
Synthesis of the positive strand of HBV DNA. Upon activation by kinases, the drug can be incorporated into the DNA which has the ultimate effect of inhibiting the HBV polymerase activity.

Dosage & Administration
The recommended dose of Entecavir for chronic hepatitis B virus infection in nucleoside-treatment-naive adults and adolescents 16 years of age is 0.5 mg once daily. For Lamivudine-refractory or known Lamivudine or Telbivudine resistance mutations, the recommended dose of Entecavir is 1 mg once daily. For patients with decompensated liver disease (adult) the recommended dose of Entecavir is 1 mg once daily. Entecavir should be administered on an empty stomach (at least 2 hours after a meal or 2 hours before the next meal).

Missed Dose: If it is almost time for next dose, skip the missed dose and take the next dose at the proper time. Nobody should take a double dose to make up for the missed dose.

Interaction
Co-administration of Entecavir with Lamivudine or Adefovir dipivoxil did not result in significant drug interactions. The effects of co-administration of Entecavir with other drugs that are eliminated through renal or are known to affect renal function have not been evaluated and patients should be monitored closely for adverse events when coadministered with such drugs.

Contraindications
Entecavir is contraindicated in patients with previously demonstrated hypersensitivity to Entecavir or any component of the product.

Side Effects
The most common adverse events are headache, fatigue, dizziness and nausea.

Pregnancy & Lactation
There are no data on the effect of Entecavir on the transmission of HBV from mother to infant. Therefore, appropriate care should be taken. It is not known whether it is excreted in human milk. Mothers should be instructed not to breastfeed if they are taking Entecavir.

Precautions & Warnings
Lactic acidosis: Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases have been reported with the use of nucleoside analogues alone or in combination with antiretrovirals.

Exacerbations of hepatitis after discontinuation of treatment: Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued anti-hepatitis B therapy, including Entecavir.

Use in Special Populations
Pediatric: Safety and effectiveness of Entecavir in pediatric patients below the age of 2 years have not been established.
Geriatric: Clinical studies of Entecavir did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. But care should be taken in dose selection, and it may be useful to monitor renal function.
Dose adjustment in renal impairment: Dose adjustment is recommended for patients with CrCl <50 ml/min including patients on hemodialysis or continuous ambulatory peritoneal dialysis (CAPD) as shown below:

CrCl ≥50 ml/min: 0.5 mg every 24 hours
CrCl 30 to <50 ml/min: 0.5 mg every 48 hours
CrCl 10 to <30 ml/min: 0.5 mg every 72 hours
CrCl <10 ml/min or Hemodialysis or CAPD: 0.5 mg every 7 days

Overdose Effects
There is no experience of Entecavir overdosage reported in patients. Healthy subjects who received up to 20 mg daily for up to 14 days and single doses up to 40 mg had no unexpected adverse events. If overdosage occurs, the patient must be monitored for evidence of toxicity and standard supportive treatment as necessary.

Storage
Keep in a dry place and store below 30°C. Protect from light and keep out of the reach of children.

Pregnancy Drug Index - Find out which medicine to give to a pregnant woman

Pregnancy Drug Index

Find out which medicine to give to a pregnant woman

We are often afraid of prescribing drugs to pregnant mothers when they go to the doctor Because most of the drugs we know are harmful to pregnancy !!

With this problem in mind, I'm trying to give you a list of what drugs can or can't be given during pregnancy from the US FDA's pregnancy index.

Let's not know the pregnancy categories before 6.

The US FDA divides drug prescription during pregnancy into 6 categories -

1) Category A:

These drugs do not pose a significant risk to fetuses after direct study of the pregnant mother.

2) Category B:

Drugs in this category have not been tested in humans, but animal trials have shown no adverse effects on fetuses. Drugs of this category can also be safely given to pregnant mothers

3) Category C:

Drugs in this category have been found to have adverse effects in animal studies (teratogenic/embryo dal/anything else). But there is no human trial with these drugs It would not be right to prescribe without calculating the risk-benefit ratio

4) Category D:

Drugs in this category have been found to have direct evidence of human fetal risk, but are acceptable if no other alternative drug is found to save the life of the pregnant mother.

5) Category X:

These drugs are completely teratogenic

6) Category N:

There have been no human or animal trials with this drug yet

Let's take a look at the pregnancy categories of conventional drugs:

* Vitamins:

1) Thiamine HCl ………………………… A
2) Folic acid …………………………… ...A

* Anti-hypertensive:

1) Methyldopa ............................................ B
2) Atenolol ……………………………......D
3) Misoprostol ………………………….....X
4) Losartan ……………………………......C
5) losartan + Thiazide ……………............. C + D

* Anti-platelets:

1) Clopidogrel …………………………….B
2) Clopidogrel + Aspirin …………….........B + D

* Anti-histamine:

1) Ketotifen ……………………………....C
2) cetirizine …………………………....... B
3) Ambroxol HCl ………………………...N

* Anti-Bacterial:

1) Penicillin ……………………………… .B
2) Amoxicillin …………………………… .B
3) Co-amoxiclav ………………………… .B
4) Flucloxacillon ………………………… B
5) Meropenem …………………………… B
(All penicillins are ..category
6) All cefalosporins are ……………….......B
7) Ciprofloxacin ………………………… ..C
8) ofloxacin ………………………………..C
9) Levofloxacin ……………………………C
10) Moxifloxacin ……………………….....C
11) Lomefloxacin ………………………....C
12) Gatifloxacin …………………………..C
13) Sparfloxacin …………………………..C
14) Gemifloxacin ……………………….....C
15) Nalidixic Acid C
16) Chloramphenicol (even drop)… C
18) Tetracyclines ……………………….....D
19) Clindamycin ………………………… B
20) Azithromycin ………………………....B
21) Erythromycin ………………………... B
22) Clarithromycin ………………………..C
23) Gentamicin …………………………....C
24) Neomycin ……………..........topical….C
25) Metronidazole ………………………...A
26) Sulfonamides ……………………….....D
27) Rifampicin..............................................C
28) Dapsone ................................................C
29) INH C ....................................................C
30) Pyraziname.............................................C
31) Ethambutol …………………………....B
32) Streptomycin ……………………….....D

* Anti Fungal:

1) Fluconazole................................................C
2) Ketoconazole .............................................C
3) Itraconazole ...............................................C
4) Miconazole ...............................................C
5) Nystatin ......................................................C
6) Clotrimazole ...............................................C
7) Amphotericin B............................................B

* Anti Viral:

1) Acyclovir ……………………………......B
2) Valacyclovir ……………………………. B
3) Adefovir ………………………………....C
4) Lamivudine ……………………………...C
5) Zidovudine …………………………….....C
6) Nelfinavir ………………………………...B
7) Abacavir ………………………………….C

* Antiprotozoal:

1) Nitazoxanide ………………………….....B
2) Artemether ……………………………… D
3) Lumefantrine …………………………....D
4) Quinine ………………………………….C
5) chloroquine ……. (Maybe safe).................N

* Anti Helminthic:

1) Albendazole …………………………......C
2) Mebendazole ………………………….....C
3) Pyrantel pamoate......................................C

* Anti Ectoparasite:

1) Permethrin ……… .topical ………… B

* Anti-Ulcerant:

1) Ranitidine ………………………… ..B
2) Omeprazole ……………………….....C
3) Pantoprazole …………………….......B
4) Rabiprazole ………………………....B
5) Lansoprazole ……………………......B
6) Esomeprazole Mg ………………......B
7) esomeprazole strontium …….............C
8) Antacids (Calcium carbonate) ............C
9) Almunium hydroxide...........................N
10) Mg (OH) 2 ………………………....N
11) Simethicone ………………………...C
12) Sucralfate …………………………..B

* Anti Spasmodic:

1) Tiemonium methyl sulfate..................N
2) Dotaverine.............................................C
3) Tramadol HCl .......................................C

* Laxative:

1) Lactulose …………………………......B

* Nausea, Vomiting, and Vertigo:

1) Cinnarone …………………………..............C
2) Meclizine ………………………....….....… B
3) Meclizine + pyridoxine ………...............… B
4) Promethazine ………………………...........C
5) Cyclizine ………………………………..... B
6) Doxylamine ………………………… ..B

* Severe Vomiting:

1) Domperidone ..........................................N
2) Ondansetron ………......…………......... B
3) Granisetron …………………………......B
4) Palonosetron ………………………........B

* NSAIDs:

1) Paracetamol ………………………......B
2) Aspirin ……………………………….C + D
3) Aceclofenac ………………………......N
4) Diclofenac …………………………...C + D
5) Ibuprofen …………………………….C + D
6) Indomethacin ……………………….. C + D
7) Naproxen …………………………......C
8) Ketorolac ……………………………...C
9) Meloxicam ………………………........C + D
10) Sulindac ……………………………...C
11) Etoricoxib ............................................N

* DMARDs:

1) Methotrexate ………………………...X
2) Azathioprine ………………………...D
3) Salfasalazine ………………………...B
4) Leflunomide .......................................X

* Muscle Relaxant:

1) Baclofen ……………………..............C
2) Tolperisone ………………..................N
3) Eperisone …………….........................N
4) Tizanidine ………………………… ..C

* Anti-cancer drugs:

1) Actinomycin ……………………… ..D
2) Busulfan. …………………………… D
3) Chlorambucil ……………………… D
4) Cyclophosphamide ……………........D
5) Doxorubicin ………………………....D
6) Mercaptopurine …………………......D
7) Methotrexate ………………………..X
8) Vinblastine …………………………...D
9) Vincristine ……………………….......D

(C + D means, these drugs are in Category C in one trimester and in Category D in one trimester)

[A = can be safely prescribed

B = can be prescribed

C = Risk-Benefit Ratio should be calculated and prescribed (this drug is harmful to the baby and pregnancy)

D = Cannot be prescribed if you want a healthy baby and pregnancy (the only life-saving conditions can be given where there is no alternative)

X = cross mark, cannot be given]

Problems related to pregnancy in category C may be -

spontaneous abortions, delayed onset of labor,

premature closing of the fetal ductus arteriosus,

jaundice, occasionally maternal (intrapartum and postpartum) and/or neonatal hemorrhage, necrotizing enterocolitis, and oligohydramnios.

Problems in category D will be:

Congenital malformations (eg, fetal growth restriction, mandibular hypoplasia, cleft palate, cranial dysostosis, spinal defects).

Enoxaparin Sodium: Uses, Dosage, Side Effects

Generic Name

Enoxaparin Sodium

Therapeutic Class: Parenteral anti-coagulants

Indications
Enoxaparin is indicated in:

Treatment of deep vein thrombosis, with or without pulmonary embolism.
Treatment of unstable angina and non-Q-wave myocardial infarction, administered concurrently with aspirin.
Prevention of thrombus formation in the extra-corporal circulation during haemodialysis.
Prophylaxis of venous thromboembolic disease (prevention of blood clot formation in the veins), in particular those which may be associated with orthopedic or general surgery.
Prophylaxis of venous thromboembolic disease in medical patients bedridden due to acute illness, including cardiac insufficiency, respiratory failure, severe infections, rheumatic diseases.

Composition
Each 0.2 ml pre-filled syringe contains Enoxaparin Sodium BP 20 mg equivalent to 2000 anti-Xa III.
Each 0.4 ml pre-filled syringe contains Enoxaparin Sodium BP 40 mg equivalent to 4000 anti-Xa III.
Each 0.6 ml pre-filled syringe contains Enoxaparin Sodium BP 60 mg equivalent to 6000 anti-Xa IU.
Each 0.8 ml pre-filled syringe contains Enoxaparin Sodium BP 80 mg equivalent to 8000 anti-Xa IU.

Pharmacology
Enoxaparin Sodium is a low molecular weight heparin with a high anti-Xa activity and low anti-lla or antithrombin activity. At doses required for the various indications, Enoxaparin Sodium does not increase bleeding time. At preventive doses, Enoxaparin Sodium causes no notable modification of activated Partial Thromboplastin Time (aPTT). It neither influences platelet aggregation nor binding of fibrinogen to platelets. Enoxaparin Sodium is primarily metabolised in the liver.

Dosage
Treatment of deep vein thrombosis, with or without pulmonary embolism: Subcutaneously 100 anti-Xa lU/kg twice daily for 10 days or Subcutaneously 150 anti-Xa lU/kq once daily for 10 days. Oral anticoagulant therapy should be initiated when appropriate and Enoxaparin Sodium treatment should be continued until a therapeutic anticoaqulant effect has been achieved.

Treatment of unstable angina and non-Q-wave myocardial infarction, administered concurrently with aspirin: Subcutaneously 100 anti-Xa lU/kg twice daily for 2- 8 days. Should be administered concurrently with oral aspirin (100 to 325 mg once daily). Treatment with Enoxaparin Sodium in these patients should be prescribed fora minimum of 2 days and continued until clinical stabilization.

Prevention of thrombus formation in extra corporeal circulation during hemodialysis:

Recommended dose is 100 anti-Xa lU/kg. For patients with a high risk of hemorrhage, the dose should be reduced to 50 anti-Xa lU/kg for double vascular access or 75 anti-Xa lU/kg for single vascular access. During hemodialysis, Enoxaparin Sodium should be introduced into the arterial line of the circuit at the beqinninq of the dialysis session.

Prophylaxis of venous thromboembolic disease in surgical patients:
Patients undergoing general surgery with a moderate risk of thromboembolism (e.g. abdominal surgery): Subcutaneously 2000 anti-Xa IU (0.2 ml) or 4000 anti-Xa IU (0.4 ml) once daily for 7 to 10 days. The first injection should be given 2 hours before the surgical procedure.

Patients undergoing orthopedic surgery with a high risk of thromboembolism: Subcutaneously 4000 anti-Xa IU (0.4 ml) once daily for 7 to 10 days. The first injection should be given 12 hours before the surgical procedure. Longer treatment duration may be appropriate in some patients like continued therapy with 4000 anti-Xa IU once daily for 3 weeks following the initial therapy has been proven to be beneficial in orthopaedic surqery.

Prophylaxis of venous thromboembolic disease in medical patients: Subcutaneously 4000 anti-Xa IU (0.4 ml) once daily for 6- 14 days.

Administration
Instructions on injecting yourself with Enoxaparin Sodium Syringes: Preparing the injection site:

Choose an area on the right or left side of your stomach. This should be at least 5 centimeters away from your belly button and out towards your sides.
Do not inject yourself within 5cm of your belly button or around existing scars or bruises.
Change the place where you inject between the left and right sides of your stomach, depending on the area you last injected.
Wash your hands. Cleanse (do not rub) the area that you will inject with an alcohol swab or soap and water.
Sit or lie in a comfortable position so that you are relaxed. Make sure you can see the place you are going to inject. A lounge chair, recliner, or bed propped up with pillows is ideal.

Selecting your dose:

Carefully pull off the needle cap from the syringe. Throw away the cap.
Do not press on the plunger before injecting yourself to get rid of air bubbles. This can lead to a loss of the medicine.
Once you have removed the cap, do not allow the needle to touch anything. This is to make sure the needle stays clean (sterile).
When the amount of medication in the syringe matches your prescribed dose, there is no need to adjust the dose. You are now ready to inject.
When the dose depends on your body weight, you may need to adjust the dose in the syringe to match the prescribed dose. In that case, you can get rid of any extra medicine by holding the syringe pointing down (to keep the air bubble in the syringe) and ejecting the extra amount into a container.
A drop may appear at the tip of the needle. If this occurs, remove the drop before injecting by tapping on the syringe with the needle pointing down. You are now ready to inject.

Injecting:

Hold the syringe in the hand you write with (like a pencil). With your other hand, gently pinch the cleaned area of your stomach between your forefinger and thumb to make a fold in the skin.
Make sure you hold the skin fold throughout the injection.
Hold the syringe so that the needle is point in straight down (vertically at a 90° angle). Insert the full length of the needle into the skin fold.
Press down on the plunger with your thumb. This will send the medication into the fatty tissue of the stomach. Complete the injection using all of the medicine in the syringe.

When you have finished:

To avoid bruising, do not rub the injection site after you have injected yourself.
Drop the used syringe into a sharps container. Close the container lid tightly and place the container out of reach of the children. When the container is full, dispose of it as your doctor or pharmacist has instructed. Any unused medicine or waste material should be disposed of in accordance with local requirements.

Interaction
It is recommended that agents which affect hemostasis should be discontinued prior to Enoxaparin Sodium therapy unless strictly indicated. These agents include medications such as: acetylsalicylic acid (and derivatives), NSAIDs (including ketorolac), ticlopidine,clopidogrel,dextran 40,glucocorticoids, thrombolytics and anticoagulants, other antiplatelet aggregation agents including glycoprotein llb/llla antagonists. If the combination is indicated, should be used with careful clinical and laboratory monitoring.

Contraindications
Patients with known hypersensitivity to Enoxaparin Sodium, heparin or other low molecular weight heparins. Patients with active major bleeding and conditions with a high risk of uncontrolled hemorrhage including recent hemorrhagic stroke.

Side Effects
Haemorrhage (bleeding), Thrombocytopenia, elevations of serum aminotransferase. Pain, bluish marks at injection sites to skin rash at injection sites. Cases of neuraxial hematomas with the concurrent use of Enoxaparin and spinal/epidural anesthesia or spinal puncture have resulted in varying degrees of neurologic injuries.

Pregnancy & Lactation
Pregnancy category B. In humans, there is no evidence that Enoxaparin Sodium crosses the placental barrier. As there are no adequate and well-controlled studies in pregnant women, Enoxaparin Sodium should be used during pregnancy only if clearly needed. Pregnant women with mechanical prosthetic heart valves may be at a higher risk for thromboembolism.

It is not known whether Enoxaparin is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue Enoxaparin, taking into account the importance of Enoxaparin to the mother and the known benefits of nursing.

Precautions & Warnings
Enoxaparin Sodium should be injected by deep subcutaneous route in prophylactic and curative treatment and by intravascular route during hemodialysis. Do not administer by the intramuscular route. Enoxaparin Sodium should be used with caution in conditions with increased potential for bleeding, such as impaired hemostasis, history of peptic ulcer, recent ischemic stroke, uncontrolled severe arterial hypertension, diabetic retinopathy and recent neuro- or ophthalmologic surgery, concomitant use of medications affecting hemostasis. It is recommended that the platelet counts be measured before the initiation of the treatment and regularly thereafter during treatment.

Use in Special Populations

Dose in Elderly Patients: No dosage adjustment is necessary, unless kidney function is impaired.
Dose in Renal Impairment: Although no dosage adjustment is recommended in patients with moderate (creatinine clearance: 30-50 ml/min) and mild (creatinine clearance: 50 80 ml/min) renal impairment, all such patients should be observed carefully for signs and symptoms of bleeding. For patients with severe (creatinine clearance <30 ml/min) renal impairment, following dosage adjustments are recommended: Prophylactic dose ranges: 2000 antiXa IU once daily; Therapeutic dose ranges: 100 anti-Xa lU/kg once daily.
Dose in Hepatic Impairment: Caution should be used in hepatically impaired patients.

Overdose Effects
Accidental overdosage following administration of Enoxaparin may lead to hemorrhagic complications. Injected Enoxaparin may be largely neutralized by the slow i.v. injection of protamine sulfate (1% solution) The dose of protamine sulfate should be equal to the dose of Enoxaparin injected: 1 mg protamine sulfate should be administered to neutralize 1 mg Enoxaparin.

Storage

Store in a cool and dry place, protect from light and moisture. Do not store above 25°C. Do not store in a refrigerator or freezer. Keep out of the reach of children

Empagliflozin + Linagliptin: Uses, Dosage, Side Effects

Generic Name

Empagliflozin + Linagliptin

Therapeutic Class: Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

Indications
This preparation is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Pharmacology
Linagliptin inhibits DPP-4 enzyme which declines the incretin hormones glucagon-like peptide-1(GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.

Empagliflozin is an inhibitor of Sodium-glucose co-transporter 2 (SGLT2). SGLT2 is the predominant transporter responsible for reabsorption of glucose from kidney back into the circulation. By inhibiting SGLT2, Empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.

Dosage & Administration
Recommended dose: 10 mg Empagliflozin and 5 mg Linagliptin once daily, taken in the morning, with or without food.

Increased dose: Dose may be increased to 25 mg Empagliflozin and 5 mg Linagliptin once daily.
Renal impaired patients: Assess renal function before initiating this tablet. Do not initiate this tablet if eGFR is below 45 mL/min/1.73 m2. Discontinue taking this tablet if eGFR falls below 45 ml/min/1.73 m2

Interaction
Diuretics: Coadministration of Empagliflozin with diuretics resulted in increased urine volume and frequency of voids, which might enhance the potential for volume depletion.

Insulin or Insulin Secretagogues: Coadministration of Empagliflozin with Insulin or Insulin secretagogues increases the risk for hypoglycemia.
Inducers of P-glycoprotein or CYP3A4 Enzymes: Rifampin decreased Linagliptin exposure, suggesting that the efficacy of Linagliptin may be reduced when administered in combination with a strong P-gp or CYP3A4 inducer.
Positive Urine Glucose Test: SGLT2 inhibitors increase urinary glucose excretion and will lead to positive urine glucose tests.
Interference with 1,5-anhydroglucitol (1,5-AG) Assay: Measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking SGLT2 inhibitors.
Inducers of P-glycoprotein or CYP3A4 Enzymes: Rifampin decreased linagliptin exposure, suggesting that the efficacy of linagliptin may be reduced when administered in combination with a strong P-gp or CYP3A4 inducer.

Contraindications
Severe renal impairment, end-stage renal disease, or dialysis
History of hypersensitivity reaction to Linagliptin, such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity
History of serious hypersensitivity reaction to Empagliflozin.

Side Effects
The following important adverse reactions are described below and elsewhere in the labeling: Pancreatitis, Ketoacidosis, Volume Depletion, Urosepsis and Pyelonephritis, Hypoglycemia with Concomitant Use with Insulin and Insulin Secretagogues, Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene), Genital Mycotic Infections, Hypersensitivity Reactions, Severe and Disabling Arthralgia, Bullous Pemphigoid. Heart Failure.

Pregnancy & Lactation
This is not recommended during the second and third trimesters of pregnancy. The limited available data of this tablet in pregnant women are not sufficient to determine a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy.

Precautions & Warnings
Precaution should be taken in some disease conditions like Pancreatitis, Hypotension, Ketoacidosis, Acute kidney injury and impairment in renal function, Urosepsis and Pyelonephritis, Hypoglycemia, Genital Mycotic Infections, Hypersensitivity etc.

Pancreatitis: Acute pancreatitis, including fatal pancreatitis, has been reported in patients treated with Linagliptin.
Ketoacidosis: Reports of ketoacidosis, a serious life-threatening condition requiring urgent hospitalization have been identified in clinical trials and postmarketing surveillance in patients with type 1 and type 2 diabetes mellitus receiving sodium glucose co-transporter-2 (SGLT2) inhibitors, including Empagliflozin. Fatal cases of ketoacidosis have been reported in patients taking Empagliflozin.
Volume Depletion: Empagliflozin can cause intravascular volume depletion which may sometimes manifest as symptomatic hypotension or acute transient changes in creatinine.
Urosepsis and Pyelonephritis: There have been postmarketing reports of serious urinary tract infections including urosepsis and pyelonephritis requiring hospitalization in patients receiving SGLT2 inhibitors, including Empagliflozin. Treatment with SGLT2 inhibitors increases the risk for urinary tract infections.
Hypoglycemia with Concomitant Use with Insulin & Insulin Secretagogues: Insulin and insulin secretagogues are known to cause hypoglycemia.
Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene): Reports of necrotizing fasciitis of the perineum (Fournier’s gangrene), a rare but serious and life-threatening necrotizing infection requiring urgent surgical intervention, have been identified in postmarketing surveillance in patients with diabetes mellitus receiving SGLT2 inhibitors, including Empagliflozin.
Genital Mycotic Infections: Empagliflozin increases the risk for genital mycotic infections. • Hypersensitivity Reactions. Severe and Disabling Arthralgia Bullous Pemphigoid.
Heart Failure: An association between DPP-4 inhibitor treatment and heart failure has been observed in cardiovascular outcomes trials for two other members of the DPP-4 inhibitor class. These trials evaluated patients with type 2 diabetes mellitus and atherosclerotic cardiovascular disease.

Overdose Effects
In the event of an overdose with this tablet, contact Poison Control Center. Employ the usual supportive measures (e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive treatment) as dictated by the patient’s clinical status. Removal of Empagliflozin by hemodialysis has not been studied, and removal of Linagliptin by hemodialysis or peritoneal dialysis is unlikely.

Storage
Store below 30° C temperature. Keep away from light and wet place. Keep out of reach of children.

Elagolix Sodium: Uses, Dosage, Side Effects

Generic Name

Elagolix Sodium

Therapeutic Class: Gonadotropin-releasing hormone (GnRH) antagonist

Indications
Elagolix is indicated for the management of moderate to severe pain associated with endometriosis.

Pharmacology
Elagolix is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of Elagolix results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones, estradiol and progesterone.

Dosage & Administration
Pregnancy should be excluded before starting treatment with Elagolix and start Elagolix within 7 days from the onset of menses.

Initial treatment with Elagolix 150 mg: 150 mg once daily up to 24 months. But in case of moderate hepatic impairment up to 6 months.

Initial treatment with Elagolix 200 mg: 200 mg twice daily up to 6 months (with coexisting dyspareunia). Treatment with Elagolix 200 mg should not exist more than 6 months as it may decrease bone mineral density (BMD).

In moderate to severe hepatic impairment: Elagolix 200 mg is not recommended.

Use in children and adolescents: <18 years not established.

Interaction
With medicine: May potentiate P-gp substrates (e.g. digoxin), CYP2C19 substrates (e.g. omeprazole; limit doses to <40 mg daily). May antagonize CYP3A substrates. Antagonizes oral midazolam, rosuvastatin; consider increasing their doses. May be antagonized by CYP3A inducers. Reduced efficacy with estrogen-containing contraceptives.

With food and others: No known food interaction.

Contraindications
It is contraindicated in pregnant women because exposure to Elagolix early in pregnancy may increase the risk of early pregnancy loss. With known osteoporosis, it can increase the risk of further bone loss. It is also contraindicated for severe hepatic impairment and also with concomitant use of strong organic anion transporting polypeptide OATP1B1 inhibitors (e.g. cyclosporine and gemfibrozil).

Side Effects
Common: The most common side effects include hot flushes, night sweats, headache, nausea, amenorrhea, , arthralgia, mood changes & bone loss. Rare: Insomnia, anxiety & elevated hepatic transaminase.

Pregnancy & Lactation
The limited human data with the use of Elagolix in pregnant women are insufficient to determine whether there is a risk for major birth defects or miscarriage. Exposure to Elagolix early in pregnancy may increase the risk of early pregnancy loss. Use of it is contraindicated in pregnant women. Elagolix has to be discontinued if pregnancy occurs during treatment. There is no information on the presence of elagolix or its metabolites in human milk, the effects on the breastfed child or the effects on milk production.

Precautions & Warnings
Bone Loss: Dose and duration-dependent decreases in bone mineral density (BMD) that may not be completely reversible. Assess BMD in women with additional risk factors for bone loss.

Reduced Ability to Recognize Pregnancy: Elagolix may alter menstrual bleeding, which may reduce the ability to recognize pregnancy. Perform testing if pregnancy is suspected. Discontinue if pregnancy is confirmed.

Suicidal Ideation and Mood Disorders: Advise patients to seek medical attention for suicidal ideation, suicidal behavior, new onset or worsening depression, anxiety, or other mood changes.

Hepatic Transaminase Elevations: Dose-dependent elevations in serum alanine aminotransferase (ALT). Counsel patients on signs and symptoms of liver injury.

Potential for Reduced Efficacy with Estrogen-Containing Contraceptives: Use non-hormonal contraception during treatment and for one week after discontinuing Elagolix.

Use in Special Populations
No dose adjustment of Elagolix is required in women with any degree of renal impairment or end-stage renal disease (including women on dialysis)
No dosage adjustment of Elagolix is required in women with mild hepatic impairment.
Safety and effectiveness of Elagolix in patients less than 18 years of age have not been established.

Overdose Effects
In case of overdose, patients should be monitored for any signs or symptoms of adverse reactions and initiate appropriate symptomatic treatment, as needed.

Storage
Store in a cool & dry place, protect from light & moisture. Keep all medicines out of reach of children.

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