Endocrine Pharmacology

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Rapid acting Insulin:

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Lispro,Aspart, Glulisine

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Short acting insulin:

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Regular

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Intermediate acting insulin:

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NPH (Neutral Protamine Hagedorn)

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Long acting insulin:

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Glargine, Detemir

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Class of Detemir

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Long acting insulin

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Class of Glargine

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Long acting insulin

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Class of NPH

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Intermediate acting insulin

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Class of Regular

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Short acting insulin

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Class of Glulisine

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rapid-acting insulin

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Class of Aspart

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rapid-acting insulin

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Class of Lispro

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rapid-acting insulin

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Clinical use of Insulin:

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Type l DM, type 2 DM,gestational diabetes, lifethreateninghyperkalemia,and stress-inducedhyperglycemia

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clinical use of which drug: Type l DM, type 2 DM,gestational diabetes, lifethreateninghyperkalemia,and stress-inducedhyperglycemia

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insulin

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Adverse reactions to insulin:

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Hypoglycemia, very rarelyhypersensitivity reactions

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Adverse reaction of which drug: Hypoglycemia, very rarelyhypersensitivity reactions.

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insulin

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MOA of insulin:

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Bind insulin receptor (tyrosinekinase activity).Liver: inc. glucose stored as glycogen.Muscle: inc. glycogen and proteinsynthesis, inc. K+ uptake.Fat: aids TG storage

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MOA of which drug: Liver: inc. glucose stored as glycogen. Muscle: inc. glycogen and protein synthesis, K+ uptake. Fat: aids TG storage

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insulin

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Name the Biguanide

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Metformin

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class of Metformin:

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Biguanide

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route of administration of metformin:

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oral

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desirable effects of metformin:

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􀂀dec. gluconeogenesis, inc. glycolysis, inc. peripheral glucose uptake(insulin sensitivity)

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desirable effects of which drug: 􀂀 dec. gluconeogenesis, inc. glycolysis, inc. peripheral glucose uptake(insulin sensitivity)

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Metformin

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Clinical use of Metformin:

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First-line therapy intype 2 DM.

Can be used in patientswithout islet function

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clinical use of which drug: First-line therapy intype 2 DM

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metformin

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Adverse effects of metformin:

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GI upset; most seriousadverse effect islactic acidosis (thuscontraindicated in renalfailure).

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adverse effects of which drug: GI upset; most seriousadverse effect islactic acidosis (thuscontraindicated in renalfailure).

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Metformin

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First generation sulfonylureas:

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Tolbutamide, Chlorpropamide

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Second generation sulfonylureas:

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Glyburide, Glimepiride, Glipizide

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class of Glipizide

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Second generation sulfonylurea

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class of glimepiride

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Second generation sulfonylurea

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class of Glyburide

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Second generation sulfonylurea

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class of Tolbutamide

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first generation sulfonylurea

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class of chlorpropamide

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first generation sulfonylurea

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MOA of sulfonylureas:

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Close K+ channel in beta-cellmembrane, so cell depolarizes-> triggering of insulin release via inc. Ca2+ influx.

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MOA of which drug: Close K+ channel in beta-cell membrane, so cell depolarizes -> triggering of insulin release via inc. Ca2+ influx.

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sulfonylurea

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name the five sulfonylureas:

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First Gen: TolbutamideChlorpropamide

Second Gen: GlyburideGlimepirideGlipizide

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Clinical use of sulfonylureas:

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Stimulate release of endogenous insulin in type 2 DM

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which drugs' clinical use Stimulate release of endogenous insulin in type 2 DM

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sulfonylureas

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difference between 1st and 2nd gen sulfonylureas:

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difference adv. effects:

First generation : disulfiram likeeffects.

Second generation :hypoglycaemia

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adverse effects of tolbutamide and chlorpropamide:

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1st gen sulfonylureas: disulfiram likeeffects.

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adverse effects of GlyburideGlimepirideGlipizide:

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2nd gen sulfonylureas: hypoglycaemia.

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which drugs' adverse effects: disulfiram like effects:

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1st gen sulfonylureas

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which drugs' adverse effects: hypoglycaemia

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2nd gen sulfonylureas

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another name for glitazones:

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thiazolidinediones

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another name for thiazolidinediones:

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glitazones

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class of Pioglitazone:

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thiazolideniones. aka glitazones

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class of rosiglitazone:

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thiazolidinediones aka glitazones

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name the thiazolideniones:

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Pioglitazone, Rosiglitazone

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MOA of the glitazones:

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Pioglitazone and Rosiglitazone:

inc. insulin sensitivity in peripheraltissue. Binds to PPAR-gamma nucleartranscription regulator...

(Genes activated by PPAR-gamma regulate fatty acid storage and glucose metabolism. Activation of PPAR-gamma inc. insulin sensitivity andlevels of adiponectin)

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MOA of which drugs: inc. insulin sensitivity in peripheraltissue. Binds to PPAR-gamama nucleartranscription regulator

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glitazones: Pioglitazone and Rosiglitazone

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clinical use of pioglitazone/rosiglitazone:

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Used as monotherapy in type2 DM or combined withabove agents

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adverse effects of the glitazones:

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Weight gain, edema, Hepatotoxicity, heart failure

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adverse effects of which drugs: Weight gain, edema, Hepatotoxicity, heart failure

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PioglitazoneRosiglitazone

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name the alpha-glucosidaseinhibitors:

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Acarbose, Miglitol

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class of Acarbose:

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alpha-glucosidase inhibitor

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class of Miglitol:

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alpha-glucosidase inhibitor

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MOA of acarbose and miglitol:

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alpha-glucosidase inhibitors:

Inhibit intestinal brush-borderalpha-glucosidases.Delayed sugar hydrolysisand glucose absorption-> dec. 􀂀 postprandial hyperglycemia

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MOA of which drugs: Inhibit intestinal brush-border alpha-glucosidases. Delayed sugar hydrolysis and glucose absorption -> dec. 􀂀 postprandial hyperglycemia.

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acarbose and miglitol

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clinical use of acarbose and miglitol:

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alpha-glucosidaseinhibitors: Used as monotherapy in type2 DM or combined withabove agents.

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adverse effects of acarbose and miglitol:

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GI disturbances

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adverse effects of which drug: GI disturbances:

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acarbose and miglitol

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name the amylin analogs:

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Pramlintide

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class of Pramlintide:

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amylin analog

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MOA of pramlintide:

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Dec. glucagon

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MOA of which drug: dec. glucagon

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amylin analog: pramlintide

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clinical use of pramlintide:

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Type l and type 2 DM.

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clinical use of which drug: Type l and type 2 DM.

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pramlintide: the amylin analog.

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adverse effects of pramlintide:

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Hypoglycemia,nausea, diarrhea

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adverse effects of which drug: Hypoglycemia,nausea, diarrhea

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pramlintide

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name the GLP-1 analogs:

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Exenatide, Liraglutide

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class of Exenatide:

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GLP-1 analog

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class of Liraglutide

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GLP-1 analog

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MOA of GLP-1 analogs:

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inc. insulin dec. glucagon release

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MOA of which drugs: inc. insulin dec. glucagon release:

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GLP-1 analogs: ExenatideLiraglutide

DPP-4 inhibitors: Linagliptin, Saxagliptin, Sitagliptin

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clinical use of Exenatide, Liraglutide:

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Type 2 DM.

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Adverse effects ofExenatide, Liraglutide:

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Nausea, vomiting;pancreatitis

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Adverse effects of which drugs: Nausea, vomiting;pancreatitis

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GLP-1 analogs: Exenatide, Liraglutide

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name the DPP-4 inhibitors:

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Linagliptin, Saxagliptin, Sitagliptin

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MOA of Linagliptin, Saxagliptin, Sitagliptin:

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DPP-4 inhibitors: inc. insulin, dec. glucose

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clinical use of DPP-4 inhibitors:

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Linagliptin, Saxagliptin, Sitagliptin:

T2DM

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adverse effects of which drugs: Mild urinary or respiratoryinfections

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DPP-4 inhibitors: Linagliptin, Saxagliptin, Sitagliptin:

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adverse effects of Linagliptin, Saxagliptin, Sitagliptin:

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DPP-4 inhibitors: Mild urinary or respiratoryinfections.

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MOA of propylthiouracil:

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Block peroxidase, thereby inhibiting organification of iodide and coupling of thyroid hormonesynthesis.

Propylthiouracil also blocks 5 '-deiodinase, which 􀂀peripheral conversion of T4 to T3 .

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MOA of methimazole:

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Block peroxidase, thereby inhibiting organification of iodide and coupling of thyroid hormone synthesis.

doesn't have PTU's effect of inhibiting 5'-deiodionase peripherally

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Clinical use of which drugs: hyperthyroidism

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Propylthiouracil. methimazole

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clinical use of Propylthiouracil. methimazole:

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hyperthyroidism

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adverse effects of Propylthiouracil:

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Skin rash, agranulocytosis (rare), aplastic anemia, hepatotoxicity propylthiouracil

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adverse effects of methimazole:

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Skin rash, agranulocytosis (rare), aplastic anemia, possible teratogen

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adverse effects of which drug specifically: Skin rash, agranulocytosis (rare), aplastic anemia, hepatotoxicity

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propylthiouracil

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adverse effects of which drug specifically: Skin rash, agranulocytosis (rare), aplastic anemia, possible teratogen

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methimazole

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MOA of Levothyroxine, triiodothyronine:

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Thyroxine replacement

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Clinical use of Levothyroxine, triiodothyronine

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Hypothyroidism, myxedema.

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MOA of which drug: thyroxine replacement:

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Levothyroxine, triiodothyronine

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clinical use of which drugs: Hypothyroidism, myxedema

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Levothyroxine, triiodothyronine

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adverse effects of which drugs: Tachycardia, heat intolerance, tremors, arrhythmias

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Levothyroxine. triiodothyronine

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adverse effects of Levothyroxine. triiodothyronine

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Tachycardia, heat intolerance, tremors, arrhythmias.

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Clinical use of which drug: GH deficiency, Turner syndrome.

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GH

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Clinical use of GH:

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GH deficiency, Turner syndrome.

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Clinical use of Somatostatin/Octreotide:

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Acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices

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Clinical use of which drug: Acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices

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Somatostatin/Octreotide

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Clinical use of which drug: Stimulates labor, uterine contractions, milk let-down; controls uterine hemorrhage

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Oxytocin

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Clinical use of Oxytocin:

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Stimulates labor, uterine contractions, milk let-down; controls uterine hemorrhage

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clinical use of which drug: Central Diabetes Insipidus

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ADH/Desmopressin

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clinical use of ADH/Desmopressin:

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Central Diabetes Insipidus

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MOA of Demeclocycline:

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ADH antagonist (member of the tetracycline family)

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MOA of which drug: ADH antagonist

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Demeclocycline

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Clinical use of Demeclocycline:

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SIADH

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Clinical use of which drug: SIADH

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Demeclocycline (ADH Antag.)

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adverse effects of Demeclocycline:

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Nephrogenic DI, photosensitivity, abnormalities of bone and teeth (tetracycline)

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name the glucocorticoids:

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Hydrocortisone, prednisone, triamcinolone, dexamethasone, beclomethasone

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class of hydrocortisone

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glucocorticoid

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class of prednisone

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glucocorticoid

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class of triamcinolone

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glucocorticoid

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class of dexamethasone

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glucocorticoid

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class of beclomethosone

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glucocorticoid

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MOA of glucocorticoids:

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􀂀 dec. production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expressionof COX-2

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clinical use of glucocorticoids:

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Addison's disease, inflammation, immune suppression, asthma

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clinical use of which drugs: Addison's disease, inflammation, immune suppression, asthma.

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glucocorticoids

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adverse effects of glucocorticoids:

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Iatrogenic Cushing's syndrome -buffalo hump, moon facies, truncal obesity, muscle wasting, thinskin, easy bruisability, osteoporosis, adrenocortical atrophy, peptic ulcers, diabetes (if chronic).

Adrenal insufficiency when drug stopped abruptly after chronic use.

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adverse effects of which drugs: Iatrogenic Cushing's syndrome -buffalo hump, moon facies, truncal obesity, muscle wasting, thinskin, easy bruisability, osteoporosis, adrenocortical atrophy, peptic ulcers, diabetes

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glucocorticoids: Hydrocortisone, prednisone, triamcinolone, dexamethasone, beclomethasone