Tuesday, November 15, 2011

Coreg Drug Description

Carvedilol is a nonselective β-adrenergic blocking agent with α1-blocking activity. It is (±)-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol. Carvedilol is a racemic mixture with the following structure:
COREG® (carvedilol)  Structural Formula Illustration
COREG (carvedilol) is a white, oval, film-coated tablet containing 3.125 mg, 6.25 mg, 12.5 mg, or 25 mg of carvedilol. The 6.25 mg, 12.5 mg, and 25 mg tablets are TILTAB® tablets. Inactive ingredients consist of colloidal silicon dioxide, Kamagra crospovidone, hypromellose, lactose, magnesium stearate, polyethylene glycol, polysorbate 80, povidone, sucrose, and titanium dioxide.
Carvedilol is a white to off-white powder with a molecular weight of 406.5 and a molecular formula of C24H26N2O4. It is freely soluble in dimethylsulfoxide; soluble in methylene chloride and methanol; sparingly soluble in 95% ethanol and isopropanol; slightly soluble in ethyl ether; and practically insoluble in water, gastric fluid (simulated, TS, pH 1.1), and intestinal fluid (simulated, TS without pancreatin, pH 7.5).
SIDE EFFECTS:See also Warning and Precautions sections.
Dizziness, lightheadedness, drowsiness, diarrhea, or tiredness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
To lower your risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position. The risk of dizziness is highest within 1 hour after you take your dose. Dizziness is most common when you first start using this drug or any time your doctor increases your dose.
This drug may reduce blood flow to your hands and feet, causing them to feel cold. Smoking may worsen this effect. Dress warmly and avoid tobacco use.
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 unlikely but serious side effects occur: very slow heartbeat, severe dizziness, fainting, unusual weakness, new or increased shortness of breath, sudden weight gain, swelling hands/ankles/feet, increased thirst/urination, numbness/tingling of the hands/feet, bluish fingers/toes.
Tell your doctor immediately if any of these rare but very serious side effects occur: change in the amount of urine, easy bruising/bleeding, mental/mood changes (e.g., depression, nervousness), 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 carvedilol, tell your doctor or pharmacist if you are allergic to it; or if you have had a serious reaction to other beta blockers (e.g., propranolol); 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.
This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: asthma, certain types of heart rhythm problems (sinus bradycardia, sick sinus syndrome, second- or third-degree atrioventricular block), severe heart failure.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, serious reaction/allergy needing treatment with epinephrine, other breathing problems (e.g., bronchitis, emphysema), other heart problems (e.g., Prinzmetal's variant angina), diabetes, overactive thyroid disease (hyperthyroidism), kidney disease, blood circulation problems (e.g., Raynaud's disease, peripheral vascular disease), a certain type of tumor (pheochromocytoma), mental/mood disorders (e.g., depression), a certain muscle disease (myasthenia gravis).
Before having surgery (including cataract eye surgery), tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
This drug may make you dizzy or drowsy or cause you to faint. This is most likely to occur within 1 hour after taking your dose or any time your doctor increases your dose. 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.
If you have diabetes, this product may prevent the fast/pounding heartbeat you would usually feel when your blood sugar level falls too low (hypoglycemia). Other symptoms of a low blood sugar level, such as dizziness and sweating, are unaffected by this drug. This product also may make it harder to control your blood sugar levels. Check your blood sugar levels regularly as directed by your doctor. Tell your doctor immediately if you have symptoms of high blood sugar such as increased thirst, hunger, and urination. Your anti-diabetic medication or diet may need to be adjusted.
Caution is advised when using this drug in older adults because they may be more sensitive to its effects, especially dizziness and lightheadedness.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
Based on information from related drugs, this medication may pass into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breast-feeding.

Flamel Gets Upbeat News About Coreg

When a drugmaker's future is so dependent on one compound, its shares are bound to be volatile whenever news about that drug comes out. Yesterday, shares of Flamel Technologies (Nasdaq: FLML) jumped more than 13% after partner GlaxoSmithKline(NYSE: GSK) announced sales numbers for Coreg CR (controlled release).
Flamel gets royalties from sales of heart-disease drug Coreg CR, which it helped develop. Flamel shares had slumped this year over concerns about the sales growth of the drug, which Glaxo had hoped would capture a good portion of the lost sales when Coreg CR's immediate release (IR) brother started facing generic competition in September.
Following a slower launch than expected this year, Glaxo yesterday announced that sales of Coreg CR were $62 million in the third quarter compared with the $20 million the drug brought in during the second quarter.
When I last wrote about Flamel, my forecast, based on historical comparisons, was that the drugmaker was likely bringing in 3% of all sales of Coreg CR as royalty revenue. Last quarter, Flamel recorded $800,000 of "other revenue." My Kamagra Chewable assumption is that $200,000 of this "other revenue" is from sources outside of Coreg CR because Flamel was recording "other revenue" in the $200,000 range for part of 2006.
If you subtract $200,000 from Flamel's first-quarter "other revenue" of $1.1 million and $200,000 from its second-quarter "other revenue" of $800,000, it brings Flamel's Coreg CR royalty revenue to $900,000 and $600,000 for the first and second quarters, respectively.
Glaxo took in $27 million in sales from Coreg CR in the first quarter and the $20 million in the second quarter. Using these two sales figures as the denominator means that Flamel took in exactly 3% in royalties in each of the first two quarters (depending on rounding and any possible lag between sales and the recording of royalties).
If you choose to ascribe all of the "other revenue" to Coreg CR royalties rather than subtracting $200,000, that puts Flamel's royalty figure at about 4% through the first two quarters. While the difference in dollars doesn't matter at this point, the royalty percentage would matter significantly to Flamel's valuation if Coreg CR sales become more substantial.
If the 3% royalty holds up, that means Flamel would bring in about $1.9 million at most in royalty revenue in the third quarter, considering the $62 million Glaxo posted in Coreg CR sales for the quarter. That's much better than last quarter's royalty revenue figure, but a far cry from profitability, considering the $23 million loss that Flamel experienced in just the first half of the year.  
On its conference call, Glaxo ratcheted down expectations for Coreg CR and said that its sales uptake would be slower than that of other controlled-release drugs like it and partnerBiovail's (NYSE: BVF) Wellbutrin XR.
Nothing that came out of the Glaxo earnings release from yesterday really changes the Coreg CR and Flamel stories. Barring strong results from a hypertension study, it looks like Coreg CR will be a shell of the $1.4 billion that Coreg IR brought in last year, and Flamel's royalty revenue will be much less than previous expectations.