Drugs Used in Diabetes Mellitus Flashcards
what is Type 3 Diabetes Mellitus
Refers to multiple other specific causes of an elevated blood glucose.
what is Type 4 Diabetes Mellitus
Gestational diabetes (GDM)
- During pregnancy, the placenta and placental hormone create an insulin resistance at 3rd trimester
what is the treatment for Type 3 Diabetes Mellitus.
insulin
what is the treatment for Type 4 Diabetes Mellitus.
insulin
MOA of insulin
tyrosine kinase phosphorylation promotes entry
of glucose into the cell
The standard mode of insulin therapy is ________injection
subcutaneous (SC)
which drugs is categorized as rapid acting insulin
Lispro
Aspart
Glulisine
tallest curve
which drugs is categorized as short acting insulin
Regular (SC/IV)
subcutaneous (SC)injection.
IV: Intravenous; NPH: Neutral Protamine Hegedorn.
which drugs is categorized as intermediate acting insulin
NPH
which drugs is categorized as LONG acting insulin
Glargine
Detemir
Degludec
flatest curve
Afrezza is an ____ form of insulin
inhaled -Powdered human insulin
Insulin powder is aerosolized and delivered to the lungs .
what do you give to treat fruity breath odor of acetone
give insulin drip until acetone goes away
how do you treat DKA
IV insulin (regular)
IV fluids, Dextrose
Correct electrolytes, K+
symptoms of hypoglycemia (<70 mg/dL)
“TIREDD”
T- tachy
-i - irritability
r- restless
E- excessive hunger
d- depressed
d- diaphoresis
Insulin allergy is mediated via
anti insulin IgE-mediated
local cutaneous reactions, angioedema, urticaria
Immune insulin resistance is mediated via
IgG antibodies
neutralize the action of insulin
Neuroglycopenic symptoms: Difficulty in
concentrating, confusion, weakness, drowsiness, a feeling
of warmth, dizziness, blurred vision, and loss of
consciousness
is seen in what glucose levels
:(<40 mg/dL)
lipoatrophy is due to
Atrophy of
subcutaneous fat at the site of insulin injection
what is lipohypertrophy
lipohypertrophy (enlargement of subcutaneous fat
depots)
if glucose is low counter regulatory hormones kicks in to raise it . those are :
glucagon
growth hormone
cortisol
epnephrine
what is the MOA of glucagon
lucagon molecule bind to specific Gs protein-coupled
receptors on liver and heart → increase in cAMP → hyperglycemia & inotropic and chronotropic effect on the heart without requiring functioning beta-adrenergic receptors.
what are the adverse effects of glucagon
Nausea
what are the uses for glucagon
Severe hypoglycemia
- glucagon injection
Endocrine diagnosis
Beta adrenergic receptor blocker overdose
- Ability to increase cAMP production in the heart
Radiology of bowel
- Relaxes the intestine
- Used in radiology as an aid to X-ray visualization
what type of category are: sulfonylureas & Glitinides
Insulin secretagogues
what type of category are: Biguanides & Thiazolidinediones
insulin sensitizers
what type of category are: Acarbose & Miglitol
alpha- glucosidase inhibitors
what type of category are: Sitagliptin & saxagliptin
DPP-4 inhbitors
what type of category are: Exenatide & Liraglutide
GLP-1 analogs
what type of category are: Pramlintide
Amlyin analogs
what type of category are: Canagliflozin
SGLTT inhbitors
what type of category are: Canagliflozin
SGLTT inhbitors
what are Sulfonylureas first generations?
FirsT-generation
Tolbutamide
Tolazamide
Chlorpropramide
what are Sulfonylureas second generations?
second Generation
↓
Glipizide
Glyburide
Glimepiride
what are some use for Second Generation Sulfonylureas
- To control hyperglycemia in type 2 DM patients who
cannot achieve appropriate control with changes in
diet alone - Most effective when pancreatic ß cells are functioning
- Most appropriate in non-obese
what are some Adverse effects of Sulfonylureas
Hypoglycemia
Severe hypoglycemia
- Overdose
- Most common with glyburide
Weight gain, Rashes, hypersensitivity
how can you tell if someone is taking Glipizide
- making more iinsulin
- c-peptide is increased
- antibodies are absent
how do you test if someone is ingesting sulphonyurea
perform urine sulphonylurea
MOA of Repaglinide, Nateglinide (D-phenylalanine)
(no sulfur)
- Meglitinides
Binds to 2 common sites of SUR, one unique site of
meglitinides on beta cells of pancreas
– Closure of ATP-sensitive K+ channels
– Restoration of more normal insulin secretion
– Glucagon secretion & hepatic glucose production
Rapid onset and short duration of action
Taken just before meals
what are some use for Repaglinide, Nateglinide (D-phenylalanine) (no sulfur)
Alone or with biguanides in type 2 diabetes & pts with S or SU allergy
which drug is safe in renal insufficency
Nateglinide is safe in renal insufficiency & lower incidence of hypoglycemia
MOA of metformin (biguanides)
**Inhibits hepatic glucose production **(through the activation of enzyme AMP-activated protein kinase (AMPK).
Inhibits mitochondrial Glycerol-3-phosphate dehydrogenase
Decreases renal gluconeogenisis
Direct stimulation of glycolysis in tissues,
Converts glucose to lactate by enterocytes
Increases removal of glucose form blood
** Increases the hepatic sensitivity **to insulin
Reduction of plasma glucagon levels
Slowing the glucose absorption from GIT
dec. Triglycerides
what are some uses for metformin
Appropriate for obese Type 2 diabetics
Decreases Insulin resistance
what are the side effects for metformin
-Anorexia, nausea, vomiting, diarrhoea
-Lactic acidosis ( inc. Blood lactate & anion gap, dec. pH, dec. HCO3)
(Anion gap= [Na+ ] – ([Cl- ] + [HCO3])
-Vitamin B 12 deficiency
what are the contraindication in metformin
Alcoholism
Renal and hepatic disease
Chronic cardiopulmonary dysfunction
Radiographic contrast studies, seriously ill patients,
Metabolic acidosis
what are the contraindication in metformin
Alcoholism
Renal and hepatic disease
Chronic cardiopulmonary dysfunction
Radiographic contrast studies, seriously ill patients,
Metabolic acidosis
what is the MOA of Thiazolidinediones:
Pioglitazone & Rosiglitazone
Pioglitazone activates PPAR-γ & PPAR-α → Upregulation of adiponectin & fatty acid uptake → Triglyceride lowering
activity (PPAR-α)
Decreases hepatic gluconeogenesis
Decreases insulin resistance [increases insulin sensitivity]
what are the adverse effects of Thiazolidinediones
- Fluid retention, edema, increased risk of heart
failure. - Weight gain, loss of bone mineral density - atypical
extremity bone fractures in women - Rosiglitazone carry more risk of Cardiovascular than Pio
- Hepatotoxicity (Troglitazone discontinued to use by
FDA
what are the contraindications of Thiazolidinediones
- Patients with a history of heart failure
- Active liver disease (or elevated transaminase levels) -
due to increased risk of hepatic injury
what is the MOA for Acarbose, Miglitol
- Inhibitor of α-glucosidase in the brush borders of
small intestine & inhibits amylase - Delay carbohydrate digestion and absorption
- Decreased demand for insulin
what is the clinical uses for Acarbose, Miglitol
control postprandial hyperglycemia
what is the adverse effects for Acarbose, Miglitol
GI discomfort, Flatulence, Diarrhea, &
hepatotoxicity
what is the adverse effects for Pramlintide
hypoglycemia
what is the MOA for Pramlintide
Suppresses glucagon release, delays gastric
emptying, and has central nervous system-mediated
anorectic effects
what are the uses for Pramlintide
Modulates postprandial glucose levels →
Preprandial use in individuals with type 1 and type 2
diabetes.
A synthetic analog of amylin given by injection is
pramlintide
what is the MOA of EXENATIDE, Liraglutide
A synthetic analog of glucagon-like-polypeptide 1 (GLP-1)
Adjunctive therapy with metformin or sulfonylureas
Potentiation of glucose-mediated insulin secretion,
Decreases glucagon release
Slowed gastric emptying, increase satiety, loss of appetite
Increased beta cell mass result from decreased beta cell
apoptosis
what are the side effects of EXENATIDE, Liraglutide
Nausea, hypoglycemia with sulfonylureas
Necrotizing & hemorrhagic pancreatitis
what is the MOA of SITAGLIPTIN, Saxagliptin
Inhibitor of dipeptidyl peptidase-4 (DPP-4)
Inhibiting the inactivation of GLP-1
Increase levels of GLP-1, GIP – increasing glucose
mediated insulin secretion and decreasing glucagon
levels
what are the adverse effects of SITAGLIPTIN, Saxagliptin
Naso-pharyngitis, upper respiratory infections, head
aches, hypoglycemia, acute pancreatitis, joint pain.
what are the MOA of Canagliflozin, Dapagliflozin, Empagliflozin
SGLT2- inhibitors-inhibits glucose reabsorption
in PCT → decrease blood glucose
what are the side effects of Canagliflozin, Dapagliflozin, Empagliflozin
hypotension/dehydration, & genital mycotic
infections, hyperkalemia, weight loss
what are the contraindications of Canagliflozin, Dapagliflozin, Empagliflozin
severe renal impairment
what is the MOA of Colesevelam
decreased Farnesoid X receptor (FXR) activation
-FXR is a nuclear receptor with multiple effects
on cholesterol, glucose & bile acid metabolism.
-Decrease glucose absorption
dec. HbA1c by 0.5%, LDL by 15%
what is the side effects of Colesevelam
Constipation, Indigestion & flatulance
what is the C/I of Colesevelam
Hypertriglyceridemia, pacreatitis,
esophagial, gastric & duodenal disorders
list the anti-obesity drug names
Orlistat, Lercaserin, Phenteramine/topiramate, Bupropionnaltrexone
what is the MOA of Orlistat
Alters fat digestion by inhibiting pancreatic lipases.
In hypertensive patients, orlistat improves blood pressure (likely
due to weight loss)
what is the adverse effects of Orlistat
GI upset; cramps, flatus, fecal incontinence, oily spotting, and
flatus with discharge
Renal – Oxalate-induced acute kidney injury has also been
reported in orlistat users
what is the contraindications of Orlistat
not be used during pregnancy or in patients with
chronic malabsorption, cholestasis, or a history of calcium oxalate
stones.
what is the MOA of Phentermine, diethylpropion, benzphetamine, phendimetrazine
Stimulate the release of norepinephrine or inhibit its reuptake
into nerve terminals, and sympathomimetic drugs reduce food intake by causing early satiety.
what is the adverse effects of Phentermine, diethylpropion, benzphetamine, phendimetrazine
All sympathomimetic drugs can increase heart rate
and blood pressure and cause insomnia, dry mouth, constipation, and nervousness.
what is the MOA of Lorcaserin
is a selective agonist of the serotonin 2C receptor. It reduces appetite and thereby reduces body weight in men and women
what is the adverse effects of Lorcaserin
Headache, upper respiratory infections,
nasopharyngitis, dizziness, and nausea
what is the contraindications of Lorcaserin
should not be used in individuals with
CrCl <30 mL/min. It is contraindicated during pregnancy
what are the drug interactions for Lorcaserin
lorcaserin should not be used with other serotonergic drugs *
(ex :SSRI’S, SNRI’S, bupropion, TCA’s, and monamine oxidase inhibitors), because of the theoretical potential for **serotonin syndrome*