Detailed description page of THPdb

Details of Th1140 which contains 1 entries.

Entry 1
(1) Primary information
ID 1634
ThPP ID Th1140
Therapeutic Peptide/Protein Name Insulin,isophane
Sequence A chain: GIVEQCCTSICSLYQLENYCN B chain: FVNQHLCGS view full sequnce in fasta
Functional Classification Ia
Molecular Weight 5808
Chemical Formula C257H383N65O77S6
Isoelectric Point 9
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life N.A.
Description Recombinant (E.coli derived), Intermediate-acting insulin to improve glycemic control. It consists of a crystalline suspension of human insulin with protamine and zinc, which results in an intermediate-acting insulin with a slower onset of action and longer duration of activity compared to regular human insulin.
Indication/Disease Used to improve glycemic control in patients with type 1 or type 2 diabetes mellitus.
Pharmacodynamics When 0.3 Units/kg of NPH insulin was subcutaneously administered, the onset of action was approximately 0.8 hours. The duration of action was 13.2 hours. The peak activity of NPH insulin occurs 4-6 hours post-dose. Compared to insulin glargine, NPH insulin has a quicker onset of action and shorter duration of action.
Mechanism of Action The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver. Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism and catabolism
Toxicity Hypoglycemia is one of the most frequent adverse events experienced by insulin users.
Metabolism Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process.
Absorption NPH insulin is generally well and rapidly absorbed from the site of injection. Absorption does not differ if it is subcutaneously administered in the thigh or abdomen. when 0.5 IU/kg of NPH insulin was given to adult type 1 diabetes patients before breakfast, the pharmacokinetic parameters are as follows: AUC (0-24hours) = 111,941 Â± 77,941 pmol Â· l-1 Â· min-1; Cmax = 149 Â± 121 pmol/l; Tmax = 480 Â± 237 minute. It is important to note that NPH insulin has a high degree of patient variability in its absorption profile.
Volume of Distribution 0.15 L/kg
Clearance N.A.
Categories Hypoglycemic Agents and Antidiabetic Agents
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target Insulin receptor
Information of corresponding available drug in the market
Brand Name Novolin N
Company Novo Nordisk
Brand Discription It is an intermediate-acting insulin administered to control blood sugar level in diabetic patient. It was created by adding neutral protamine to regular procine insulin. Insulin isophane is a man-made form of a hormone that is produced in the body. It works by lowering levels of glucose (sugar) in the blood. Insulin isophane is a long-acting form of insulin that is slightly different from other forms of insulin that are not man-made. Insulin isophane is used to treat diabetes. Insulin isophane may also be used for purposes not listed in this medication guide. This package contains Novolin N in an InnoLet disposable prefilled insulin syringe. Novolin N is commonly known as NPH, Human Insulin Isophane Suspension (recombinant DNA origin). The concentration of this product is 100 units of insulin per milliliter. It is a cloudy or milky suspension of human insulin with protamine and zinc. The insulin substance (the cloudy material) settles at the bottom of the insulin reservoir, therefore, the Novolin N InnoLet (nph, human insulin isophane suspension 3 ml disposable prefilled syringe) must be rotated up and down so that the contents are uniformly mixed before a dose is given. Novolin N has an intermediate duration of action. The effect of Novolin N begins approximately 1Â½ hours after injection. The effect is maximal between 4 and 12 hours. The full duration of action may last up to 24 hours after injection. The time course of action of any insulin may vary considerably in different individuals, or at different times in the same individual. Because of this variation, the time periods listed here should be considered as general guidance only. This human insulin (recombinant DNA origin) is structurally identical to the insulin produced by the human pancreas. This human insulin is produced by recombinant DNA technology utilizing Saccharomyces cerevisiae (bakers' yeast) as the production organism.
Prescribed for Type 1 Diabetes Mellitus, Type 2 Diabetes Mellitus,
Chemical Name N.A.
Formulation Novolin N in an InnoLet disposable prefilled insulin syringe. Novolin N is commonly known as NPH, Human Insulin Isophane Suspension (recombinant DNA origin). The concentration of this product is 100 units of insulin per milliliter. It is a cloudy or milky suspension of human insulin with protamine and zinc. The insulin substance (the cloudy material) settles at the bottom of the insulin reservoir, therefore, the Novolin N InnoLet (nph, human insulin isophane suspension 3 ml disposable prefilled syringe) must be rotated up and down so that the contents are uniformly mixed before a dose is given
Physcial Appearance Novolin N InnoLet (nph, human insulin isophane suspension 3 ml disposable prefilled syringe)
Route of Administration Subcutaneous
Recommended Dosage 0.5 U/kg/day SC (Type 1 Diabetes Mellitus), 0.5-1 units/kg/day in divided doses (Type 2 Diabetes Mellitus)
Contraindication Tell your doctor or pharmacist if you have any medical conditions, pregnant, planning to become pregnant, or are breast-feeding; taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement; allergies to medicines, foods, or other substances; drink alcoholic beverages or smoke; heart problems (eg, heart failure); kidney or liver problems; nerve problems; adrenal, pituitary, or thyroid problems; or diabetic ketoacidosis; use 3 or more insulin injections per day; if you are fasting, have high blood sodium levels, or are on a low-salt (sodium) diet. Some MEDICINES MAY INTERACT with insulin isophane vials. Tell your health care provider if you are taking any other medicines, especially any of the following: Beta-blockers, Angiotensin-converting enzyme, (ACE) inhibitors, Thiazolidinediones Corticosteroids .
Side Effects insulin allergy, Hypoglycemia, or low blood sugar, is the most common side effect of insulin. Symptoms of low blood sugar may include headache, hunger, sweating, pale skin, irritability, dizziness, feeling shaky, or trouble concentrating. Watch for signs of low blood sugar. Carry a piece of non-dietetic hard candy or glucose tablets with you in case you have low blood sugar. Tell your doctor if you have itching, swelling, redness, or thickening of the skin where you inject insulin isophane.
Useful Link http://en.wikipedia.org/wiki/NPH_insulin http://www.drugs.com/mtm/insulin-isophane.html http://reference.medscape.com/drug/humulin-70-30-novolin-70-30-insulin-isophane-human-insulin-regular-human-999708
PubMed ID US4430266
3-D Structure Th1140 A chainor (Download)Th1140 B chain (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

(1) Primary information
Entry 1
ID	1634
ThPP ID	Th1140
Therapeutic Peptide/Protein Name	Insulin,isophane
Sequence	A chain: GIVEQCCTSICSLYQLENYCN B chain: FVNQHLCGS view full sequnce in fasta
Functional Classification	Ia
Molecular Weight	5808
Chemical Formula	C257H383N65O77S6
Isoelectric Point	9
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	N.A.
Description	Recombinant (E.coli derived), Intermediate-acting insulin to improve glycemic control. It consists of a crystalline suspension of human insulin with protamine and zinc, which results in an intermediate-acting insulin with a slower onset of action and longer duration of activity compared to regular human insulin.
Indication/Disease	Used to improve glycemic control in patients with type 1 or type 2 diabetes mellitus.
Pharmacodynamics	When 0.3 Units/kg of NPH insulin was subcutaneously administered, the onset of action was approximately 0.8 hours. The duration of action was 13.2 hours. The peak activity of NPH insulin occurs 4-6 hours post-dose. Compared to insulin glargine, NPH insulin has a quicker onset of action and shorter duration of action.
Mechanism of Action	The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver. Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism and catabolism
Toxicity	Hypoglycemia is one of the most frequent adverse events experienced by insulin users.
Metabolism	Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process.
Absorption	NPH insulin is generally well and rapidly absorbed from the site of injection. Absorption does not differ if it is subcutaneously administered in the thigh or abdomen. when 0.5 IU/kg of NPH insulin was given to adult type 1 diabetes patients before breakfast, the pharmacokinetic parameters are as follows: AUC (0-24hours) = 111,941 Â± 77,941 pmol Â· l-1 Â· min-1; Cmax = 149 Â± 121 pmol/l; Tmax = 480 Â± 237 minute. It is important to note that NPH insulin has a high degree of patient variability in its absorption profile.
Volume of Distribution	0.15 L/kg
Clearance	N.A.
Categories	Hypoglycemic Agents and Antidiabetic Agents
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	Insulin receptor
Information of corresponding available drug in the market
Brand Name	Novolin N
Company	Novo Nordisk
Brand Discription	It is an intermediate-acting insulin administered to control blood sugar level in diabetic patient. It was created by adding neutral protamine to regular procine insulin. Insulin isophane is a man-made form of a hormone that is produced in the body. It works by lowering levels of glucose (sugar) in the blood. Insulin isophane is a long-acting form of insulin that is slightly different from other forms of insulin that are not man-made. Insulin isophane is used to treat diabetes. Insulin isophane may also be used for purposes not listed in this medication guide. This package contains Novolin N in an InnoLet disposable prefilled insulin syringe. Novolin N is commonly known as NPH, Human Insulin Isophane Suspension (recombinant DNA origin). The concentration of this product is 100 units of insulin per milliliter. It is a cloudy or milky suspension of human insulin with protamine and zinc. The insulin substance (the cloudy material) settles at the bottom of the insulin reservoir, therefore, the Novolin N InnoLet (nph, human insulin isophane suspension 3 ml disposable prefilled syringe) must be rotated up and down so that the contents are uniformly mixed before a dose is given. Novolin N has an intermediate duration of action. The effect of Novolin N begins approximately 1Â½ hours after injection. The effect is maximal between 4 and 12 hours. The full duration of action may last up to 24 hours after injection. The time course of action of any insulin may vary considerably in different individuals, or at different times in the same individual. Because of this variation, the time periods listed here should be considered as general guidance only. This human insulin (recombinant DNA origin) is structurally identical to the insulin produced by the human pancreas. This human insulin is produced by recombinant DNA technology utilizing Saccharomyces cerevisiae (bakers' yeast) as the production organism.
Prescribed for	Type 1 Diabetes Mellitus, Type 2 Diabetes Mellitus,
Chemical Name	N.A.
Formulation	Novolin N in an InnoLet disposable prefilled insulin syringe. Novolin N is commonly known as NPH, Human Insulin Isophane Suspension (recombinant DNA origin). The concentration of this product is 100 units of insulin per milliliter. It is a cloudy or milky suspension of human insulin with protamine and zinc. The insulin substance (the cloudy material) settles at the bottom of the insulin reservoir, therefore, the Novolin N InnoLet (nph, human insulin isophane suspension 3 ml disposable prefilled syringe) must be rotated up and down so that the contents are uniformly mixed before a dose is given
Physcial Appearance	Novolin N InnoLet (nph, human insulin isophane suspension 3 ml disposable prefilled syringe)
Route of Administration	Subcutaneous
Recommended Dosage	0.5 U/kg/day SC (Type 1 Diabetes Mellitus), 0.5-1 units/kg/day in divided doses (Type 2 Diabetes Mellitus)
Contraindication	Tell your doctor or pharmacist if you have any medical conditions, pregnant, planning to become pregnant, or are breast-feeding; taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement; allergies to medicines, foods, or other substances; drink alcoholic beverages or smoke; heart problems (eg, heart failure); kidney or liver problems; nerve problems; adrenal, pituitary, or thyroid problems; or diabetic ketoacidosis; use 3 or more insulin injections per day; if you are fasting, have high blood sodium levels, or are on a low-salt (sodium) diet. Some MEDICINES MAY INTERACT with insulin isophane vials. Tell your health care provider if you are taking any other medicines, especially any of the following: Beta-blockers, Angiotensin-converting enzyme, (ACE) inhibitors, Thiazolidinediones Corticosteroids .
Side Effects	insulin allergy, Hypoglycemia, or low blood sugar, is the most common side effect of insulin. Symptoms of low blood sugar may include headache, hunger, sweating, pale skin, irritability, dizziness, feeling shaky, or trouble concentrating. Watch for signs of low blood sugar. Carry a piece of non-dietetic hard candy or glucose tablets with you in case you have low blood sugar. Tell your doctor if you have itching, swelling, redness, or thickening of the skin where you inject insulin isophane.
Useful Link	http://en.wikipedia.org/wiki/NPH_insulin http://www.drugs.com/mtm/insulin-isophane.html http://reference.medscape.com/drug/humulin-70-30-novolin-70-30-insulin-isophane-human-insulin-regular-human-999708
PubMed ID	US4430266
3-D Structure	Th1140 A chainor (Download)Th1140 B chain (View) or (Download)