Drug Study on Buscopan

Jul 31st, 2010 by kaiastillo

Inhibits muscarinic actions of acetylcholine on autonomic effectors innervated by
postganglionic cholinergic neurons. May effect neural pathways originating in the inner
ear to inhibit nausea and vomiting.

Generic Name: Hyoscine ButylBromide

Brand Name: Buscopan

Classification: Belladona alkaloid, antimuscarinic

Indication & Dosages:

 Spastic states
Adults: 0.4 to 0.8 mg P.O.

 Delirium, preanesthetic sedation and obstetric amnesia with analgesics

Adults: 0.3 to 0.65 mg I.V., I.M., or subcutaneously. Dilute solution with sterile water for injection
before giving I.V.

Children: 0.006mg/kg I.V., I.M., or subcutaneously. Maximum dose, 0.3 mg. Dilute solution with
sterile water for solution before giving I.V.

 To prevent nausea and vomiting from motion sickness

Adults: One Transderm-Scop, formulated to deliver 1mg scopolamine over 3 days, applied to the
skin behing the ear at least 4 hours before antiemetic is needed. Or, 0.3 to 0.65 mg
hydrobromide I.V., I.M. or subcutaneously. Or, 0.25 to 0.8 mg P.O. 1 hour before exposure to
motion. Further doses of 0.25 to 0.8 mg may be given t.i.d., p.r.n.

Children: 6 mcg/k or 200 mcg hydrobromide I.V., I.m., or subcutaneously

Mode of Action:

 Inhibits muscarinic actions of acetylcholine on autonomic effectors       innervated by

postganglionic cholinergic neurons. May effect neural pathways originating in the inner ear
to inhibit nausea and vomiting.
Contraindication:

 Contraindicated in patients with angleclosure glaucoma, obstructive uropathy, obstructive

disease of the GI tract, asthma, chronic pulmonary disease, myasthenia gravis, paralytic
ileus, intestinal atony, unstable CV status in acute hemorrhage, tachycardia from cardiac
insufficiency, or toxic megacolon.
 Contraindicated in patients with hypersensitive to belladonna or barbiturates.
 Use cautiously in patients with autonomicneuropathy, hyperthyroidism, coronary artery
disease, arrhythmias, heart failure, hypertension, hiatal hernia with ferlux esophagitis,
hepatc or renal disease, known as suspected GI infection, or ulcerative colitis.
 Use cautiously in children.
 Use cautiously in patients in hot or humid environments; drug can cause heat stroke.
Side Effects:

 Frequent: Dry mouth (sometimes severe), decreased sweating, constipation.

 Occasional: Blurred vision; bloated feeling; urinary hesitancy; somnolence (with high
dosage); headache; intolerance to light; loss of taste; nervousness; flushing; insomnia;
impotence; mental confusion or excitement (particularly in the elderly and children);
temporary light-headedness (parenteral form); local irritation(with parenteral form).
Adverse Reaction:

 Overdose may produce temporary paralysis of ciliary muscle; papillary dilation;

tachycardia; palpitations; hot, dry, or flushed skin; absence of bowel sounds; hyperthermia;
increased respiratory rate; EKG abnormalities; nausea; vomiting; rash over face or upper
trunk; CNSstimulations; and psychosis (marked by agitation, restlessness, rambling speech,
visual hallucinations, paranoid behavior, and delusions, followed by depression).
Nursing Responsibilities:

 Advise patient to apply patch the night before a planned trip. Transdermal method
releases a controlled therapeutic amount of drug. Transderm-Scop is effective if applied 2 or
3 hours before experiencing motion but is more effective if applied 12 hours before.
 Instruct patient to remove one patch before applying another
 Instruct patient to wash and dry hands thoroughly before and after applying the
transdermal patch (on dry skin behind the ear) and before touching the eye because pupil
may dilate. Tell patient to discard patch after removing it and to wash application site
thoroughly.
 Tell patient that if patch becomes displaced, he should remove it and apply another patch
on a fresh skin site behind the ear.
 Alert patient to possible withdrawal signs or symptoms (nausea, vomiting, headache,
dizziness) when transdermal system is used for longer than 72 hours.
 Advice patient that eyes may be ore sensitive to light while wearing patch. Advice patient
to wear sunglasses for comfort
 Urge patient to report urinary hesitancy or urine retention.

Duvadilan® [tab]

Solvay Pharma 
MIMS Class : Drugs Acting on the Uterus 

See related Duvadilan tab (Drugs Acting on the Uterus) information

Contents Isoxsuprine HCl
Indications Prevention & treatment of premature labour & other undesired
 uterine contractions eg surgical intervention during pregnancy
& cerclage.
Dosage Immediate suppression of uterine motility 0.2-0.5 mg/min by
IV infusion or 10 mg IM 1-2 hrly. Maintenance: 20 mg 3-4 times
daily. Circulatory disturbances 20 mg orally 3-4 times daily or
10 mg parenterally 3 times daily.
Administration Should be taken with food (Take after meals to minimise GI
discomfort.).
Contraindications Recent cerebral hemorrhage.
Adverse Drug Occasional transient palpitations, fall in BP or dizziness (reduce
Reactions dose).
View ADR Monitoring Form
Pregnancy
Category (US
FDA) Category C: Either studies in animals have revealed adverse
effects on the foetus (teratogenic or embryocidal or other) and
there are no controlled studies in women or studies in women
and animals are not available. Drugs should be given only if the
potential benefit justifies the potential risk to the foetus.
MIMS Class Drugs Acting on the Uterus
ATC C04AA01 - Isoxsuprine ; Belongs to the class of 2-amino-1-
Classification phenylethanol derivative agents. Used as peripheral
vasodilators.

Isoxsuprine Hydrochloride
Pronouncation: (eye-SOX-you-preen HIGH-droe-KLOR-ide)
Class: Peripheral vasodilator

Trade Names:
Vasodilan
- Tablets 10 mg
- Tablets 20 mg

Trade Names:
Voxsuprine
- Tablets 10 mg
- Tablets 20 mg

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Pharmacology
Stimulates skeletal beta receptors to produce vasodilation; stimulates cardiac function (increased
contractility, heart rate, and cardiac output) and relaxes uterus. At higher doses, inhibits platelet
aggregation and decreases blood viscosity.

Pharmacokinetics

Absorption

Well absorbed from the GI tract.

Metabolism

Partially conjugated in the blood.

Elimination

The t 1/2 is approximately 1.25 h. Primarily excreted in the urine.

Onset

1 h (oral); 10 min (IV).

Special Populations

Neonates

The t 1/2 is 1.5 to 3 h (near term) and 6 to 8 h (for less mature).

Indications and Usage

Possibly effective for treatment of cerebral vascular insufficiency, peripheral vascular disease
caused by arteriosclerosis obliterans, thromboangiitis obliterans, Raynaud's disease.

Unlabeled Uses

Treatment of dysmenorrhea, premature labor.

Contraindications
Arterial bleeding; use during immediate postpartum period.
Dosage and Administration
Adults

PO 10 to 20 mg 3 or 4 times daily.

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Drug Interactions
None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension; tachycardia; chest pain.

CNS

Dizziness; weakness.

Dermatologic

Severe rash.

GI

Nausea; vomiting; abdominal distress.

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Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Patient Information

 Instruct patient to report the following symptoms to health care provider: Fast
heartbeat, chest pain, pounding in chest, severe rash, flushing, weakness, nausea,
vomiting, stomach pain.
 Caution patient to avoid sudden position changes to prevent orthostatic hypotension.

Methergine®
(methylergonovine maleate) Tablets, USP
(methylergonovine maleate) Injection, USP

DRUG DESCRIPTION
WHAT ARE THE POSSIBLE SIDE EFFECTS OF METHYLERGONOVINE (METHERGINE)?
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing;
swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have any of these serious side effects:

 increased blood pressure (severe headache, blurred vision);

 seizure (convulsions);
 feeling light-headed, fainting;
 pounding heartbeat;
 chest pain or heavy feeling, pain spreading to the arm or shoulder,...

Read All Potential Side Effects and See Pictures of Methergine »

Methergine® (methylergonovine maleate) is a semi-synthetic ergot alkaloid used for the prevention
and control ofpostpartum hemorrhage.

INDICATIONS
For routine management after delivery of the placenta; postpartum atony andhemorrhage;
subinvolution. Under full obstetric supervision, it may be given in thesecond stage of labor following
delivery of the anterior shoulder.

DOSAGE AND ADMINISTRATION

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to
administration.
Intramuscularly

1 mL, 0.2 mg, after delivery of the anterior shoulder, after delivery of the placenta, or during
the puerperium. May be repeated as required, at intervals of 2-4 hours.

Intravenously

Dosage same as intramuscular. (See WARNINGS.)

Orally

One tablet, 0.2 mg, 3 or 4 times daily in the puerperium for a maximum of 1 week.

SIDE EFFECTS
The most common adverse reaction is hypertension associated in several cases
with seizure and/or headache. Hypotension has also been reported. Nausea and vomiting have
occurred occasionally. Rarely observed reactions have included:acute myocardial infarction, transient
chest pains, arterial spasm (coronary and
peripheral), bradycardia, tachycardia, dyspnea, hematuria, thrombophlebitis, water intoxication,
hallucinations, leg cramps, dizziness, tinnitus, nasal congestion, diarrhea, diaphoresis, palpitation,
rash, and foul taste.1

There have been rare isolated reports of anaphylaxis, without a proven causal relationship to the drug
product.

Drug Abuse And Dependence

Methergine® (methylergonovine maleate) has not been associated with drug abuse or dependence of
either a physical or psychological nature.

WARNINGS
This drug should not be administered I.V. routinely because of the possibility of inducing
sudden hypertensive and cerebrovascular accidents. If I.V. administration is considered essential as a
lifesaving measure, Methergine® (methylergonovine maleate) should be given slowly over a period of
no less than 60 seconds with careful monitoring of blood pressure. Intra-arterial or periarterial injection
should be strictly avoided.

PRECAUTIONS
General

Caution should be exercised in the presence of sepsis,

obliterative vasculardisease, hepatic or renal involvement. Also use with caution during the second
stage of labor. The necessity for manual removal of a retained placenta should occur only rarely with
proper technique and adequate allowance of time for its spontaneous separation.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term studies have been performed in animals to evaluate carcinogenicpotential. The effect of

the drug on mutagenesis or fertility has not been determined.

Pregnancy

Category C. Animal reproductive studies have not been conducted with Methergine. It is also not
known whether methylergonovine maleate can cause fetal harm or can affect reproductive capacity.
Use of Methergine is contraindicated during pregnancy because of its uterotonic effects.
(SeeINDICATIONS AND USAGE.)
 Labor and Delivery

The uterotonic effect of Methergine is utilized after delivery to assist involution and
decrease hemorrhage, shortening the third stage of labor.

Nursing Mothers

Methergine® (methylergonovine maleate) may be administered orally for a maximum of 1

week postpartum to control uterine bleeding. Recommended dosage is 1 tablet (0.2 mg) 3 or 4 times
daily. At this dosage level a small quantity of drug appears in mothers' milk. Caution should be
exercised when Methergine is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Clinical studies of Methergine did not include sufficient number of subjects aged 65 and over to
determine whether they respond differently from younger subjects. Other reported clinical experience
has not identified differences in response between the elderly and younger patients. In general dose
selection for an elderly patient should be cautious, usually starting at the low end of the dosing range,
reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant
disease or other drug therapy.

OVERDOSE
Symptoms of acute overdose may include: nausea, vomiting, abdominal pain, numbness, tingling of
the extremities, rise in blood pressure, in severe cases followed by hypotension, respiratory
depression, hypothermia, convulsions, andcoma.

Because reports of overdosage with Methergine® (methylergonovine maleate) are infrequent,

the lethal dose in humans has not been established. The oral LD50 (in mg/kg) for the mouse is 187,
the rat 93, and the rabbit 4.5.2 Several cases of accidental Methergine injection in newborn infants
have been reported, and in such cases 0.2 mg represents an overdose of great magnitude. However,
recovery occurred in all but one case following a period of respiratory depression, hypothermia,
hypertonicity with jerking movements, and, in one case, a single convulsion.

Also, several children 1-3 years of age have accidentally ingested up to 10 tablets (2 mg) with no
apparent ill effects. A postpartum patient took 4 tablets at one time in error and reported paresthesias
and clamminess as her only symptoms.

Treatment of acute overdosage is symptomatic and includes the usual procedures of:

1. removal of offending drug by inducing emesis, gastric lavage, catharsis, and

supportive diuresis.
2. maintenance of adequate pulmonary ventilation, especially if convulsions or coma develop.
3. correction of hypotension with pressor drugs as needed.
4. control of convulsions with standard anticonvulsant agents.
5. control of peripheral vasospasm with warmth to the extremities if needed. 3

CONTRAINDICATIONS
Hypertension; toxemia; pregnancy; and hypersensitivity.
2. Berde, B. and Schild, H.O.: Ergot Alkaloids and Related Compounds, Springer-Verlag, New York, 1978, p. 810.
3.   Treatment of Acute Overdosage. Novartis Consumer Health, Inc. Rx Products. Novartis, Medical Services
Department.

CLINICAL PHARMACOLOGY
Methergine® (methylergonovine maleate) acts directly on the smooth muscle of the uterus and
increases the tone, rate, and amplitude of rhythmic contractions. Thus, it induces a rapid and
sustained tetanic uterotonic effect which shortens the third stage of labor and reduces blood loss. The
onset of action after I.V. administration is immediate; after I.M. administration, 2-5 minutes, and after
oral administration, 5-10 minutes.

Pharmacokinetic studies following an I.V. injection have shown that methylergonovine is rapidly
distributed from plasma to peripheral tissues within 2-3 minutes or less. The bioavailability after oral
administration was reported to be about 60% with no accumulation after repeated doses. During
delivery, withintramuscular injection, bioavailability increased to 78%. Ergot alkaloids are mostly
eliminated by hepatic metabolism and excretion, and the decrease in bioavailability following oral
administration is probably a result of first-pass metabolism in the liver.

Bioavailability studies conducted in fasting healthy female volunteers have shown that oral absorption
of a 0.2 mg methylergonovine tablet was fairly rapid with a mean peak plasma concentration of 3243
± 1308 pg/mL observed at 1.12 ± 0.82 hours. For a 0.2 mg intramuscular injection, a mean peak
plasma concentration of 5918 ± 1952 pg/mL was observed at 0.41 ± 0.21 hours. The extent of
absorption of the tablet, based upon methylergonovine plasma concentrations, was found to be
equivalent to that of the I.M. solution given orally, and the extent of oral absorption of the I.M. solution
was proportional to the dose following administration of 0.1, 0.2, and 0.4 mg. When given
intramuscularly, the extent of absorption of Methergine solution was about 25% greater than the
tablet. The volume of distribution (Vdss/F) of methylergonovine was calculated to be 56.1 ± 17.0 liters,
and the plasma clearance (CLp/F) was calculated to be 14.4 ± 4.5 liters per hour. The plasma level
decline was biphasic with a mean elimination half-life of 3.39 hours (range 1.5 to 12.7 hours). A
delayed gastrointestinalabsorption (Tmax about 3 hours) of Methergine tablet might be observed
inpostpartum women during continuous treatment with this oxytocic agent.

USES:This medication is used after childbirth to help stop bleeding from the uterus. Methylergonovine
belongs to a class of drugs known as ergot alkaloids. It works by increasing the rate and strength of
contractions and the stiffness of the uterus muscles. These effects help to decrease bleeding.
HOW TO USE:Take this medication by mouth with or without food, usually 3 to 4 times daily for up to
1 week after delivery or as directed by your doctor.
Dosage is based on your medical condition and response to treatment.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the
same times each day.

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor
instructs you otherwise. Grapefruit can increase the amount of this medication in your bloodstream.
Consult your doctor or pharmacist for more details.

Tell your doctor if your condition persists or worsens.

SIDE EFFECTS:Headache, nausea, vomiting, or dizziness may occur. If any of these effects persist
or worsen, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the
benefit to you is greater than the risk of side effects. Many people using this medication do not have
serious side effects.
Tell your doctor immediately if any of these rare but serious side effects occur: fast/slow heartbeat,
shortness of breath, cold hands/feet, pain/redness/swelling of arms or legs.

Seek immediate medical attention if any of these rare but serious side effects occur: chest pain, vision
changes, confusion, seizures.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you
notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the
face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact
your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA
at             1-800-FDA-1088      .

In Canada - Call your doctor for medical advice about side effects. You may report side effects to
Health Canada at             1-866-234-2345      .

PRECAUTIONS:Before taking methylergonovine, tell your doctor or pharmacist if you are allergic to it;
or to similar ergot alkaloids (such as ergonovine); or if you have any other allergies. This product may
contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your
pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney
disease, liver disease, high blood pressure, heart disease (such as venoatrial shunts, mitral valve
stenosis), blood vessel disease (such as Raynaud's disease), complications during pregnancy (such
as preeclampsia, eclampsia).

This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness
until you are sure you can perform such activities safely. Limit alcoholic beverages.

This medication must not be used during pregnancy. It may harm an unborn baby. Consult your
doctor for more details.

This medication passes into breast milk, but is unlikely to harm a nursing infant. Consult your doctor
before breast-feeding.

STORAGE:Store at room temperature below 77 degrees F (25 degrees C) away from light and
moisture. Do not store in the bathroom. Keep all medicines away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly
discard this product when it is expired or no longer needed. Consult your pharmacist or local waste
disposal company for more details about how to safely discard your product.

VITAMIN K1
INJECTION
Phytonadione
Injectable Emulsion, USP
Phytonadione is a vitamin, which is a clear, yellow to amber, viscous, odorless or nearly odorless
liquid. It is insoluble in water, soluble in chloroform and slightly soluble in ethanol.

Vitamin K1 Injection (Phytonadione Injectable Emulsion, USP) is indicated in the following coagulation
disorders which are due to faulty formation of factors II, VII, IX and X when caused by vitamin K
deficiency or interference with vitamin K activity.

Vitamin K1 Injection is indicated in:

 anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione

derivatives;

 prophylaxis and therapy of hemorrhagic disease of the newborn;

 hypoprothrombinemia due to antibacterial therapy;

 hypoprothrombinemia secondary to factors limiting absorption or synthesis of vitamin K, e.g.,

obstructive jaundice, biliary fistula, sprue, ulcerative colitis, celiac disease, intestinal resection,
cystic fibrosis of the pancreas, and regional enteritis;

 other drug-induced hypoprothrombinemia where it is definitely shown that the result is due to
interference with vitamin K metabolism, e.g., salicylates.

DOSAGE AND ADMINISTRATION

Whenever possible, Vitamin K1 Injection (Phytonadione Injectable Emulsion, USP) should be given by
the subcutaneous route. (See Box Warning.) When intravenous administration is considered
unavoidable, the drug should be injected very slowly, not exceeding 1 mg per minute.

Protect from light at all times.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to
administration, whenever solution and container permit.

Directions for Dilution

Vitamin K1 Injection may be diluted with 0.9% Sodium Chloride Injection, 5% Dextrose Injection, or
5% Dextrose and Sodium Chloride Injection. Benzyl alcohol as a preservative has been associated
with toxicity in newborns. Therefore,all of the above diluents should be preservative-free (see
WARNINGS). Other diluents should not be used. When dilutions are indicated, administration should
be started immediately after mixture with the diluent, and unused portions of the dilution should be
discarded, as well as unused contents of the ampul.

Prophylaxis of Hemorrhagic Disease of the Newborn

The American Academy of Pediatrics recommends that vitamin K1 be given to the newborn. A single
intramuscular dose of Vitamin K1 Injection 0.5 to 1 mg within one hour of birth is recommended.

Treatment of Hemorrhagic Disease of the Newborn

Empiric administration of vitamin K1 should not replace proper laboratory evaluation of the coagulation
mechanism. A prompt response (shortening of the prothrombin time in 2 to 4 hours) following
administration of vitamin K1 is usually diagnostic of hemorrhagic disease of the newborn, and failure to
respond indicates another diagnosis or coagulation disorder.
 Vitamin K1 Injection 1 mg should be given either subcutaneously or intramuscularly. Higher doses
may be necessary if the mother has been receiving oral anticoagulants.

Whole blood or component therapy may be indicated if bleeding is excessive. This therapy, however,
does not correct the underlying disorder and Vitamin K 1 Injection should be given concurrently.

Effective for:

 Treating and preventing vitamin K deficiency.

 Preventing certain bleeding or blood clotting problems.
 Reversing the effects of too much warfarin used to prevent blood clotting.
 Vitamin K is safe for most people. Most people do not experience any side effects when taking in the
recommended amount each day.

Special Precautions & Warnings:

 Pregnancy and breast-feeding: When taken in the recommended amount each day, vitamin
K is considered safe for pregnant and breast-feeding women, but don't use higher amounts
without the advice of your healthcare professional.

Kidney disease: Too much vitamin K can be harmful if you are receiving dialysis treatments
due to kidney disease.

Liver disease: Vitamin K is not effective for treating clotting problems caused by severe liver
disease. In fact, high doses of vitamin K can make clotting problems worse in these people.

MEPHYTON is indicated in the following coagulation disorders which are due to faulty formation of

factors II, VII, IX and X when caused by vitamin K deficiency or interference with vitamin K activity.

MEPHYTON tablets are indicated in:

— anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives;

— hypoprothrombinemia secondary to antibacterial therapy;

— hypoprothrombinemia secondary to administration of salicylates;

— hypoprothrombinemia secondary to obstructive jaundice or biliary fistulas but only if bile salts

are administered concurrently, since otherwise the oral vitamin K will not be absorbed

SIDE EFFECTS
Severe hypersensitivity reactions, including anaphylactoid reactions and deaths have been reported
following parenteral administration. The majority of these reported events occurred
following intravenous administration.

Transient "flushing sensations" and "peculiar" sensations of taste have been observed with parenteral
phytonadione, as well as rare instances of dizziness, rapid and weak pulse, profuse sweating,
brief hypotension, dyspnea, andcyanosis.

Hyperbilirubinemia has been observed in the newborn following administration of parenteral

phytonadione. This has occurred rarely and primarily with doses above those recommended.
WARNINGS
An immediate coagulant effect should not be expected after administration of phytonadione.

Phytonadione will not counteract the anticoagulant action of heparin.

When vitamin K1 is used to correct excessive anticoagulant-induced hypoprothrombinemia,

anticoagulant therapy still being indicated, the patient is again faced with the clotting hazards existing
prior to starting the anticoagulant therapy. Phytonadione is not a clotting agent, but overzealous
therapy with vitamin K1 may restore conditions which originally permitted thromboembolic
phenomena. Dosage should be kept as low as possible, and prothrombin timeshould be checked
regularly as clinical conditions indicate.

Repeated large doses of vitamin K are not warranted in liver disease if the response to initial use of
the vitamin is unsatisfactory. Failure to respond to vitamin K may indicate a congenital coagulation
defect or that the condition being treated is unresponsive to vitamin K.

PRECAUTIONS
General

Vitamin K1 is fairly rapidly degraded by light; therefore, always protect MEPHYTON from light. Store
MEPHYTON in closed original carton until contents have been used. (See also HOW SUPPLIED,
Storage.)

Carcinogenesis, Mutagenesis, Impairment of Fertility

Studies of carcinogenicity or impairment of fertility have not been performed with MEPHYTON.
MEPHYTON at concentrations up to 2000 mcg/plate with or without metabolic activation, was
negative in the Ames microbial mutagen test.

Pregnancy

Pregnancy Category C: Animal reproduction studies have not been conducted with MEPHYTON. It
is also not known whether MEPHYTON can cause fetal harm when administered to a pregnant
woman or can affect reproduction capacity. MEPHYTON should be given to a pregnant woman only if
clearly needed.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established with
MEPHYTON. Hemolysis, jaundice, and hyperbilirubinemia in newborns, particularly in premature
infants, have been reported with vitamin K.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in
human milk, caution should be exercised when MEPHYTON is administered to a nursing woman.

Geriatric Use

Clinical studies of MEPHYTON did not include sufficient numbers of subjects aged 65 and over to
determine whether they respond differently from younger subjects. Other reported clinical experience
has not identified differences in responses between the elderly and younger patients. In general, dose
selection for an elderly patient should be cautious, usually starting at the low end of the dosing range,
reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant
disease or other drug therapy.
OVERDOSE
The intravenous and oral LD50s in the mouse are approximately 1.17 g/kg and greater than 24.18
g/kg, respectively.

CONTRAINDICATIONS
Hypersensitivity to any component of this medication.

CLINICAL PHARMACOLOGY
MEPHYTON tablets possess the same type and degree of activity as does naturally-occurring vitamin
K, which is necessary for the production via the liverof active prothrombin (factor II), proconvertin
(factor VII), plasma thromboplastin component (factor IX), and Stuart factor (factor X). The
prothrombin test is sensitive to the levels of three of these four factors – II, VII, and X. Vitamin K is
an essential cofactor for a microsomal enzyme that catalyzes the posttranslational carboxylation of
multiple, specific, peptidebound glutamic acidresidues in inactive hepatic precursors of factors II, VII,
IX, and X. The resulting gammacarboxyglutamic acid residues convert the precursors into
activecoagulation factors that are subsequently secreted by liver cells into the blood.

Oral phytonadione is adequately absorbed from the gastrointestinal tract only ifbile salts are present.
After absorption, phytonadione is initially concentrated in the liver, but the concentration declines
rapidly. Very little vitamin K accumulates in tissues. Little is known about the metabolic fate of vitamin
K. Almost no free unmetabolized vitamin K appears in bile or urine.

In normal animals and humans, phytonadione is virtually devoid of pharmacodynamic activity.

However, in animals and humans deficient in vitamin K, the pharmacological action of vitamin K is
related to its normal physiological function; that is, to promote the hepatic biosynthesis of vitamin K-
dependent clotting factors.

MEPHYTON tablets generally exert their effect within 6 to 10 hours.

USES:Vitamin K is used to treat and prevent low levels of certain substances (blood clotting factors)
that your body naturally produces. These substances help your blood to thicken and stop bleeding
normally (e.g., after an accidental cut or injury). Low levels of blood clotting factors increase the risk
for unusual bleeding. Low levels may be caused by certain medications (e.g., warfarin) or medical
conditions (e.g., obstructive jaundice). Vitamin K helps to treat and prevent unusual bleeding by
increasing the body's production of blood clotting factors.
HOW TO USE:Take this medication by mouth exactly as directed by your doctor. Dosage is based on
your medical condition and response to treatment.
If you are using a certain "blood thinner" drug (warfarin), vitamin K can decrease the effects of
warfarin for up to 2 weeks. Therefore, be sure to take your vitamin K and warfarin exactly as directed
by your doctor or pharmacist.

If you develop easy bruising or bleeding, seek immediate medical attention. You may need another
dose of vitamin K.

SIDE EFFECTS:Vitamin K usually has very few side effects. If you have any unusual effects from
taking this medicine, tell your doctor or pharmacist promptly.
If your doctor has prescribed this medication, remember that he or she has judged that the benefit to
you is greater than the risk of side effects. Many people using this medication do not have serious
side effects.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you
notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the
face/tongue/throat), severe dizziness, trouble breathing.
PRECAUTIONS:Before taking vitamin K, tell your doctor or pharmacist if you are allergic to it; or if
you have any other allergies.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood
disorders, gallbladder disease (e.g., obstructive jaundice, biliary fistula), liver disease.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and
benefits with your doctor.

It is not known whether this medication passes into breast milk. Consult your doctor before breast-
feeding.

STORAGE:Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light
and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly
discard this product when it is expired or no longer needed. Consult your pharmacist or local waste
disposal company for more details about how to safely discard your product.

Nubain® [amp]

Invida [ Zuellig ] 
MIMS Class : Anaesthetics - Local & General, Analgesics (Opioid) 
 

See related Nubain Preservative-Free amp information

Contents Nalbuphine HCl
Indications For the relief of moderate to severe pain. Nalbuphine HCl
can also be used for preoperative analgesia, as a
supplement to balanced anesthesia, surgical anesthesia,
for obstetrical analgesia during labor and for the relief of
pain following acute myocardial infarction. Postoperative
somatic and visceral pain.
Dosage Usual Recommended Dose: Adults: 0.15-0.2 mg/kg body
weight. Children: 0.1-0.2 mg/kg up to a total single dose of
10 mg.

Nubain may be administered SC, IM or IV. The doses may

be repeated every 3-6 hrs or as needed. Dosage should be
adjusted according to severity of pain and physical status of
the patient.
Overdosage Symptoms: The administration of single IM doses of 72 mg
of nalbuphine HCl to 8 normal subjects has been reported
to have resulted primarily in symptoms of sleepiness and
mild dysphoria.

Treatment: Naloxone HCl is a specific antidote for

nalbuphine HCl, but symptomatic and supportive therapy
 will usually suffice for mild or moderate overdosage.
Oxygen, IV fluids, vasopressors and other supportive
measures should be employed as indicated.
Contraindications Patients who are hypersensitive to nalbuphine HCl.
Warnings Drug Dependence: Nalbuphine HCl cannot be substituted
for heroine, methadone or other narcotics in physically
dependent individuals. It will precipitate abstinence in such
patients. Nalbuphine HCl has been shown to have a low
abuse potential. Psychological and physical dependence
and tolerance may follow the misuse or abuse of
nalbuphine; therefore, caution should be observed in
prescribing it for emotionally unstable patients or for
individuals with a history of narcotic abuse. When
nalbuphine HCl is selected for the control of chronic pain,
care should be taken to avoid increases in dosage or the
frequency of administration which, in susceptible
individuals, might result in physical dependence and
tolerance. Abrupt withdrawal after chronic use can
precipitate abstinence syndrome.

Use in Ambulatory Patients: Nalbuphine HCl may impair the

mental or physical abilities required for the performance of
potentially dangerous tasks eg, driving a car or operating
machinery. Therefore, it should be administered with
caution to ambulatory patients who should be warned to
avoid such hazards.

Use in Pregnancy: Safe use of nalbuphine HCl in

pregnancy (other than labor) has not been established. It
should only be administered to pregnant women (other than
in labor) when, in the judgement of the physician, the
potential benefits outweigh the possible hazards. Potent
analgesics should be used with caution in women delivering
premature infants. In full-term labor, 10-15 mg of
nalbuphine has provided analgesia equivalent to that of 75-
113 mg of meperidine with fewer maternal side effects.

Use During Labor and Delivery: The placental transfer of

nalbuphine is high, rapid and variable with a maternal-to-
fetal ratio ranging from 1:0.37 to 1:1.6. Fetal and neonatal
adverse effects that have been reported following the
administration of nalbuphine to the mother during labor
include fetal tachycardia, respiratory depression at birth,
apnea and cyanosis. Maternal administration of naloxone
during labor has normalized these effects in some cases.
Severe and prolonged fetal bradycardia has been reported.
Permanent neurological damage attributed to fetal
 bradycardia has occurred. A sinusoidal fetal heart rate
pattern associated with the use of nalbuphine has also
been reported. Nubain should be used with caution in
women during labor and delivery, and newborns should be
monitored for respiratory depression, apnea, bradycardia
and arrhythmias if Nubain has been used.

Head Injury and Increased Intracranial Pressure: The

possible respiratory depressant effects and the potential of
potent analgesics to elevate cerebrospinal fluid pressure
(resulting from vasodilation following CO2 retention) may be
markedly exaggerated in the presence of head injury,
intracranial lesions or a preexisting increase in intracranial
pressure. Furthermore, potent analgesics can produce
effects which may obscure the clinical course of patients
with head injuries. Therefore, nalbuphine HCl should be
used in these circumstances only when essential, and then
should be administered with extreme caution.
Special Precautions Impaired Respiration: 10 mg of nalbuphine HCl causes
some respiratory depression approximately equivalent to 10
mg of morphine. However, in contrast to morphine,
respiratory depression is not appreciably increased with
higher doses of nalbuphine HCl. Respiratory depression
induced by nalbuphine HCl can be reversed by naloxone
HCl when indicated. It should be administered with caution
at low doses to patients with impaired respiration (eg, from
other medication, uremia, bronchial asthma, severe
infection, cyanosis or respiratory obstruction).

Impaired Renal or Hepatic Function: Because nalbuphine

HCl is metabolized in the liver and excreted by the kidneys,
patients with renal or liver dysfunction may over-react to
customary doses. Therefore, in these individuals,
nalbuphine HCl should be used with caution and
administered in reduced amounts. However, liver and renal
function tests on patients who have received nalbuphine
HCl in single and chronic dosages do not reveal any
changes attributable to its administration.

Use in pregnancy & lactation: Caution should be

exercised when administered to pregnant and nursing
patients. Nalbuphine should only be administered when in
the judgement of the physician, the potential benefits
outweigh the possible hazards (see Warnings).
Adverse Drug The most commonly occurring reactions are sedation,
Reactions drowsiness, sweating, nausea, dry mouth and dizziness.
Pain at injection site, headache, vomiting and
lightheadedness occur less frequently. Restlessness,
 blurred vision, chills, euphoria and impaired respiration
have been infrequent.

Nubain produces few if any psychotomimetic side effects

eg, visual hallucinations and dysphoria.

Monitoring on the Usage: Prescriptions of Nubain shall be

through an ordinary prescription form wherein the name,
address, S2 license number and PTR number of the
prescribing practitioner shall be stated, as well as the
name, address and age of the patient. The pharmacist must
keep a record of its sales including the name and address
of the prescribing physician in an Additional Dangerous
Drugs Record Book registered prior to use.
Click to view ADR Monitoring Website
Drug Interactions With Other Central Nervous System Depressants: Although
nalbuphine HCl possesses narcotic antagonistic activity,
there is evidence that in non-dependent patients, it will not
antagonize a narcotic analgesic administered just before,
concurrently, or just after an injection of nalbuphine HCl.
Therefore, patients receiving narcotic analgesics, general
anesthetics, phenothiazines or other tranquilizers,
sedatives, hypnotics or other CNS depressants (including
alcohol) concomitantly with nalbuphine HCl may exhibit an
additive effect. When such combined therapy is
contemplated, the dose of one or both agents should be
reduced.
View more drug interactions for Nubain
Pregnancy Category
(US FDA)
Category B: Either animal-reproduction studies have not
demonstrated a foetal risk but there are no controlled
studies in pregnant women or animal-reproduction studies
have shown an adverse effect (other than a decrease in
fertility) that was not confirmed in controlled studies in
women in the 1sttrimester (and there is no evidence of a risk
in later trimesters).
if prolonged use/high doses at
term.

Category D: There is positive evidence of human foetal

risk, but the benefits from use in pregnant women may be
acceptable despite the risk (e.g., if the drug is needed in a
life-threatening situation or for a serious disease for which
safer drugs cannot be used or are ineffective).
Storage Store at temperatures not exceeding 30°C.
Description Each mL of Nubain ampoule also contains sodium chloride
2 mg, sodium citrate 9.41 mg and anhydrous citric acid
12.62 mg; pH is adjusted with hydrochloric acid.

Nalbuphine HCl is (-)-17-(cyclobutylmethyl)-4,5α-

epoxymorphinan-3,6α,14-triol hydrochloride. It is a synthetic
agonist-antagonist analgesic of the phenanthrene series
which is chemically related to both the widely used narcotic
antagonist, naloxone, and the potent analgesic,
oxymorphone.
Mechanism of Action Pharmacology: Nalbuphine HCl is a potent analgesic, 10
mg of which is comparable in analgesic potency to 8-10 mg
of morphine sulfate, whether administered IV, SC or IM.

The onset of action occurs within 2-3 min after IV

administration of nalbuphine HCl and in <10 min following
SC or IM injection.

Clinical experience suggests that in some patients,

analgesia may be longer lasting than from comparable
doses of morphine, effects having been observed in acute
and chronic pain for 3-8 hrs. The t½ of nalbuphine is 5 hrs.

Nalbuphine HCl has the effect of lowering the cardiac work

load and can be used immediately in myocardial infarction
(use with caution where emesis is involved). Hemodynamic
studies in patients with severe arteriosclerotic heart
changes reveal that nalbuphine HCl has circulatory effects
similar to those of morphine ie, a minimal decrease in
oxygen consumption, cardiac index, left ventricular end
diastolic pressure and cardiac work.

Nalbuphine HCl antagonist activity is ¼ as potent as

nalorphine and approximately 1/40 that of naloxone.
MIMS Class Anaesthetics - Local & General / Analgesics (Opioid)
ATC Classification N02AF02 - Nalbuphine ; Belongs to the class of morphinan
derivative opioids. Used to relieve pain.
Poison Schedule Rx
Presentation/Packing Amp 10 mg/mL (preservative-free) x 1 mL x 10's, 100's.