Method for treating acute and severe diarrhea

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C514S424000

Reexamination Certificate

active

06214792

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates generally to a method for treating acute and severe diarrhea as may occur during chemotherapy or acute narcotic withdrawal. More particularly, the present invention provides such a method utilizing the somatostatin analogue octreotide.
BACKGROUND OF THE INVENTION
Acute and severe diarrhea may occur in many circumstances. However clinically significant diarrhea is commonly seen during cancer chemotherapy and during the acute phase of withdrawal in persons addicted to narcotics such as heroin and methadone.
Newer techniques for treating narcotic addiction entail purposefully precipitating an acute withdrawal reaction by the administration of narcotic antagonist drugs such as naloxone, naltrexone or nalmefene. For example, the '081 application, herein incorporated by reference, discloses rapid detoxification methods using the opioid antagonist nalmefene. As disclosed in the '081 application, the addicted patient is given a 1.0 mg intravenous bolus of nalmefene, followed by a intravenous infusion of 1.0 mg nalmefene some time after the initial bolus. Approximately 10 hours after the nalmefene is infused, another 1.0 mg dose of parenteral nalmefene may be given, such as by subcutaneous or intramuscular injection. Approximately 10 hours later a final intramuscular or subcutaneous bolus dose of nalmefene can be given, thereby completing a cycle of parenteral administration of nalmefene totaling approximately 4.0 mg over a span of time approximately 24 hours.
Alternatively, a loading dose of from about 0.5-1.5 mg to no more than about 1.5-2.0 mg is given, followed by slow intravenous infusion at a rate equivalent to 2.0-3.5 mg/day. This dosage regimen is convenient if the patient is to receive intravenous hydration for treatment of nausea and/or diarrhea as may sometimes be associated with withdrawal from opioids.
A method for treating the acute and severe diarrhea typically precipitated by rapid detoxification procedures is to administer the somatostatin analogue octreotide or lanreotide. While octreotide has proven effective in treating clinically significant diarrhea during rapid detoxification, it is associated with an unacceptable incidence of bradycardia, which in some instances has been so severe as to be life threatening.
It is, accordingly, an object of the invention to provide an effective method for treating acute and severe diarrhea
It is a further object of the invention to provide such a method which reduces the incidence of life threatening bradycardia.
It is a still further object of the invention to provide a method of rapid narcotic detoxification which safely and effectively treats the acute and severe diarrhea typically accompanying acute withdrawal.
SUMMARY OF THE INVENTION
The present invention meets the above-stated objects by providing a method for treating acute and severe diarrhea comprising the step of administering octreotide in an amount sufficient to alleviate the diarrhea without precipitating clinically significant bradycardia. Preferably octreotide is administered in a dosage of from about 3×10
−4
to about 14×10
−4
mg/kg of body weight, more preferably, in a dose of about 0.0007 mg/kg of body weight, about 0.025 mg to about 0.1 mg for a 70 kg person. Lanreotide may be administered in a therapeutically equipotent dose.
A preferred embodiment of the invention, the method comprises administering octreotide and/or lanreotide together with an anti-cholinergic such as atropine or glycopyrrolate. When administered with octreotide or lanreotide in the preferred dosage range, glycopyrrolate is administered in a dosage range of about 2×10
−4
to about 6.0×10
−3
mg/kg of body weight and more preferably, in a dosage range of about 7×10
−4
mg/kg to about 2×10
−3
mg/kg of body weight. Atropine is preferably administered in a dosage range of about 2×10
−4
mg/kg to about 6.0×10
−3
mg/kg of body weight, more preferably about 2.0×10
−3
to about 5.0×10
−3
mg/kg of body weight and yet, more preferably, about 1.4×10
−3
to 4.5×10
−3
mg/kg of body weight. In a preferred embodiment, octreotide is administered in a dosage range of 50 to 75 mcg somatostatin, glycopyrrolate 0.75 to 0.125 mg and/or atropine 0.175 to 0.225 mg, based on a 70 kg body weight. Other anti-cholinergic drugs producing similar anti-muscarinic activity with respect to acetylcholine at postganglionic parasympathetic neuroeffector sites in cardiac muscle may be substituted for atropine and/or glycopyrrolate. Lanreotide at therapeutically equipotent doses to the octreotide doses specified may be employed in lieu of the octreotide. Lanreotide may also be admixed with octreotide to form a mixture which may be employed in lieu of the octreotide or lanreotide alone. Preferably the mixture has therapeutic activity equipotent to that produced by doses of octreotide referenced herein.
In a particularly preferred embodiment of the invention, about 60 to about 75 micrograms of octreotide is combined with approximately 0.1 mg glycopyrrolate and 0.2 mg atropine. A compatible preservative may be used, such as benzyl alcohol, and pH may be adjusted to physiological levels by addition of, for example, hydrochloric acid, sodium hydroxide or sulfuric acid. Clinical experience has demonstrated an embodiment comprising 60 mg octreotide with 0.2 atropine and 0.1 mg glycopyrrolate is particularly effective when typically administered every 6 to 12 hours, most commonly every 8 to 12 hours, for a 70 kg adult human.
The proportions of atropine, octreotide and glycopyrrolate as embodied in one embodiment of the present invention may be prepared by mixing 0.5 cc of a 0.2 mg/cc concentrate of glycopyrrolate with 0.5 cc of a 0.4 mg/cc concentrate of atropine and 0.3 cc of a 200 mg/cc concentrate of sandostatin. Alternatively, 0.5 to 0.75 cc of a 100 mg/cc concentrate of octreotide can be mixed with these same amounts of atropine and glycopyrrolate.
The present invention also provides a method and apparatus for reducing the negative effects of psychological/physiological withdrawal. The method and apparatus ameliorates withdrawal symptomology by reducing the psychological “cue response” evidenced in addicts upon display of a needle-like protuberance. A cue response is elicited when a triggering event—such as seeing or being administered a syringe with a needle-like protuberance—initiates a craving for the drug previously associated cognitively or subconsciously with said syringe having the needle-like protuberance. Commonly, a human addicted to an opioid agonist drug, such a heroin, associates the effects of the drug with the sight and usage of a syringe with a needle-like protuberance. Even when heroin is not used or administered, the cue response may elicit a craving for heroin upon the mere appearance or usage of a syringe with a needle-like protuberance. According to the invention, administration of the octreotide and/or anti-cholinergic drug, and other drugs given to the addict to alleviate or ameliorate withdrawal symptoms, is performed using an injection device having a concealed needle, or which lacks a needle component. In a preferred embodiment, a needleless jet injection device is used to administer the drugs. Representative needleless injection devices finding use in the present invention are described, for example, in U.S. Pat. Nos. 5,919,159, 5,879,327, 5,704,911, 5,559,302 and 5,569,189, the disclosures of which are incorporated by reference herein.
The present invention also provides a method for rapidly detoxifying a patient addicted to exogenously administered narcotics while effectively treating the acute and severe diarrhea that typically accompanies acute withdrawal. According to the invention, acute clinical withdrawal is induced by administering at least about 0.5-1.5 mg up to about 1.5-2.0 mg of nalmefene, based on the weight of a 70 kg human. The diarrhea associated with such withdrawal is treated

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