Gadobutrol- Godavist- @- Diagnostic agents (Mar 2011)
Drug Name:Gadobutrol- Godavist- @- Diagnostic agents (Mar 2011)
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
There are no known drug interactions. Gadavist does not interfere with serum
and plasma calcium measurements determined by colorimetric assays.
Do not mix Gadavist with other drugs.
Indication:
Gadavist (gadobutrol) injection, for intravenous use
Initial U.S. Approval: 2011
WARNING: NEPHROGENIC SYSTEMIC FIBROSIS (NSF)
See full prescribing information for complete boxed warning
Gadolinium-based contrast agents (GBCAs) increase the risk for NSF among
patients with impaired elimination of the drugs. Avoid use of GBCAs in these
patients unless the diagnostic information is essential and not available with
non-contrasted MRI or other modalities.
The risk for NSF appears highest among patients with:
Chronic, severe kidney disease (GFR < 30 mL/min/1.73m2), or
Acute kidney injury.
Screen patients for acute kidney injury and other conditions that may reduce
renal function. For patients at risk for chronically reduced renal function
(for example, age >60 years, hypertension or diabetes), estimate the
glomerular filtration rate (GFR) through laboratory testing
Drug Name- Gadavist
Active Ingredient - Gadobutrol
For use in patients undergoing magnetic image resonance imaging
(MRI) of the central nervous system
Indication-
For use in patients undergoing magnetic image resonance imaging
(MRI) of the central nervous system
Approved by FDA on 14-3-2011 (Ref- FDA approved List- 2011)
LIST OF APPROVED DRUG FROM 01-01-2015 To 31-12-2015
ISSUED BY NEW DRUG DIVISION - DRUG CONTROLLER GENERAL- INDIA
Sr.No Name of Drug Indication Date of Issue
7. Gadobutrol solution for injection 07-05-2015
10mg/10mg
In adult, adolescence and children aged 2 years
and older for:
1. Contrast enhancement in cranial and spinal
magnetic resonance imaging (MRI)
2.Contrast enhancement MRI of other body regions:
liver, kidneys
3.Contrast enhancement in Magnetic Resonance
Angiography (CE-MRA)
4.For MRI of the breast to assess the presence
of malignant breast
Approved by DCG INDIA (Ref- DCGI approved List- 01-01-2015 To 31-12-3015)
Adverse Reaction:
.
The most frequent (. 0.5%) adverse reactions associated with Gadavist
in clinical studies were headache, nausea, injection site reaction,
dysgeusia and feeling hot.
Contra-Indications:
CONTRAINDICATIONS
None
WARNINGS AND PRECAUTIONS
.
Nephrogenic Systemic Fibrosis has occurred in patients with impaired
elimination of GBCAs. Higher than recommended dosing or repeated
dosing appears to increase the risk.
.
Hypersensitivity: Anaphylactoid/anaphylactic reactions with cardiovascular,
respiratory or cutaneous manifestations, ranging from mild to severe,
including death, have uncommonly occurred.
Monitor patients closely for need of emergency cardiorespiratory support.
Dosages/ Overdosage Etc:
INDICATIONS AND USAGE
Gadavist is a gadolinium-based contrast agent indicated for intravenous
use in diagnostic MRI in adults and children (2 years of age and older)
to detect and visualize areas with disrupted blood brain barrier (BBB)
and/or abnormal vascularity of the central nervous system.
DOSAGE AND ADMINISTRATION
Gadavist is formulated at a higher concentration (1 mmol/mL) compared
to certain other gadolinium-based contrast agents, resulting in a lower
volume of administration. Use the table in section 2.1 to determine
the volume of Gadavist to be administered
The recommended dose of Gadavist is 0.1 mL/kg body weight (0.1 mmol/kg),
administered as an intravenous bolus injection at a flow rate of approximately
2 mL/second. Flush the intravenous cannula with physiological saline
solution after the injection.
DOSAGE FORMS AND STRENGTHS
Gadavist injection contains 1 mmol gadobutrol/mL (equivalent to 604.72 mg
gadobutrol/mL) and is available in vials and prefilled syringes
Patient Information:
PATIENT COUNSELING INFORMATION
1. Nephrogenic Systemic Fibrosis
Instruct patients to inform their physician if they:
- Have a history of kidney disease and/or liver disease, or
-Have recently received a GBCA
GBCAs increase the risk of NSF among patients with impaired elimination of drugs.
To counsel patients at risk of NSF:
-Describe the clinical manifestation of NSF
-Describe procedures to screen for the detection of renal impairment
- Instruct the patients to contact their physician if they develop signs or symptoms
of NSF following Gadavist administration, such as burning, itching, swelling, scaling,
hardening and tightening of the skin; red or dark patches on the skin; stiffness in joints
with trouble moving, bending or straightening the arms, hands, legs or feet; pain in
the hip bones or ribs; or muscle weakness.
2. Common Adverse Reactions
Inform patients that they may experience:
-Reactions along the venous injection site, such as mild and transient burning or pain
or feeling of warmth or coldness at the injection site•
-Side effects of headache, nausea, abnormal taste and feeling hot
3. General Precautions
Instruct patients receiving Gadavist to inform their physician if they:
-Are pregnant or breastfeeding
-Have a history of allergic reaction to contrast media, bronchial asthma or
allergic respiratory disorder,
- Are taking any medications
Pharmacology/ Pharmacokinetics:
1 Mechanism of Action
In MRI, visualization of normal and pathological tissue depends in part on variations
in the radiofrequency signal intensity that occur with:
- Differences in proton density
-Differences of the spin-lattice or longitudinal relaxation times (T1)
- Differences in the spin-spin or transverse relaxation time (T2)
When placed in a magnetic field, Gadavist shortens the T1 and T2 relaxation times.
The extent of decrease of T1 and T2 relaxation times, and therefore the
amount of signal enhancement obtained from Gadavist, is based upon
several factors including the concentration of Gadavist in the tissue,
the field strength of the MRI system, and the relative ratio of the
longitudinal and transverse relaxation times.
At the recommended dose, the T1 shortening effect is observed with greatest
sensitivity in T1-weighted magnetic resonance sequences. In T2*-weighted sequences
the induction of local magnetic field inhomogeneities by the large magnetic moment
of gadolinium and at high concentrations (during bolus injection) leads to a signal decrease
2. Pharmacokinetics
Distribution
After intravenous administration, gadobutrol is rapidly distributed in the
extracellular space. After a gadobutrol dose of 0.1 mmol/kg body weight,
an average level of 0.59 mmol gadobutrol/L was measured in plasma
2 minutes after the injection and 0.3 mmol gadobutrol/L 60 minutes after the injection.
Gadobutrol does not display any particular protein binding.
In rats, gadobutrol does not penetrate the intact blood-brain barrier.
Metabolism
Gadobutrol is not metabolized.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
.1 Pregnancy
Pregnancy Category C
There are no adequate and well-controlled studies of Gadavist in pregnant women.
While it is unknown if Gadavist crosses the human placenta, other gadolinium-based
contrast agents (GBCAs) do cross the placenta in humans and result in fetal exposure.
Limited published human data on exposure to other GBCAs during pregnancy
did not show adverse effects in exposed neonates.
Gadavist should be used during pregnancy only if the potential benefit justifies
the potential risk to the fetus.
2. Nursing Mothers
It is not known whether gadobutrol is excreted in human milk.
Limited case reports on use of GBCAs in nursing mothers indicate
that 0.01 to 0.04% of the maternal gadolinium dose is excreted in human breast milk.
Studies have shown limited GBCA gastrointestinal absorption.
Nonclinical data show that gadobutrol is excreted into breast milk in very
small amounts (<0.1% of the dose intravenously administered)
and the absorption via the gastrointestinal tract is poor (approximately
5% of the dose orally administered was excreted in the urine
Because many drugs are excreted in human milk, exercise caution when
gadobutrol is administered to a nursing woman.
3.Pedeatric Use
The pharmacokinetics, safety and efficacy of Gadavist at a single dose
of 0.1 mmol/kg have been established in children 2 to 17 years of age.
No dose adjustment according to age is necessary in this population.
The safety and effectiveness of Gadavist have not been established in children
below two years of age.
4. Geriatric Use
In clinical studies of Gadavist, 1377 patients were 65 years of age and over,
while 104 patients were 80 years of age and over. No overall differences
in safety or effectiveness were observed between these subjects and
younger subjects, and other reported clinical experience has not identified
differences in responses between the elderly and younger patients.
In general, use of Gadavist in elderly patients should be cautious, reflecting
the greater frequency of impaired renal function and concomitant disease
or other drug therapy. No dose adjustment according to age is necessary
in this population
