A: 12-15 Flashcards
Thyroid preparations (2)
Levothyroxine
Iodine
Levothyroxine:
How to give?
When is the maximum effect?
Oral/IV
After 6-8 weeks
Daily requirement of Iodine
150 micro g
Iodine indications
Deficiency
Thyrotoxicosis crisis
Iodine side effects
Cutaneous and mucus membrane irritation
Allergic
Hypo/Hyper -thyroiditis
Antithyroid drugs MOA
Inhibit thyroid Peroxidase activity
Inhibit Deionidase
Antithyroid drugs (2)
Propylthiouracil (PTU)
Thi.amazole
Propylthiouracil (PTU)
Hoe to give
Duration of action
Oral
6-8 h
Propylthiouracil (PTU)
Methimazole
How long until they work? Why?
3-4 weeks
Since the realease of preformed hormones is not affected
Propylthiouracil (PTU) side effects
Skin rash GI Vasculitis Liver Hypothyroidism Lupus
Methimazole
Hoe to give
Duration of action
Oral
24 h
Which of them doesnt effect Deionidase?
Propylthiouracil (PTU)
Methimazole
Methimazole
Which of them is safe during pregnancy?
Propylthiouracil (PTU)
Methimazole
Propylthiouracil (PTU)
Methimazole side effects
Skin rash Nausea Vasculitis Agranulocytosis Liver Hypothyroidism Lupus Teratogenic
Somatostatin analoge
Octreotide
Dopamine D2-R agonist
Bromocriptine
Hypothalamic and Pituitary hormones- which drugs should I know?
Desmopresin (ADH)
Octreotide (GH antagonist)
Bromocriptine (D2-R agonis)
Oxytocin
DOB-O
Octreotide MOA
GH antaginist (Somatostatin anloge)
Octreotide indications
Control of bleeding in esophageal varices
Acromegaly
Gigantism
Endocrine tumors
CAGE
Octreotide side effects
bradycardia Cardiac conduction abnormalities GI Gall stones Steatorrhea
Why will we see Gall stones when taking Octreotide?
Impaired pancreatic secretions
Which drug can suppress pituitary excretion of prolactin?
Bromocriptine
Bromocriptine indications
Prolactin secreting adenoma
Acromegaly
Bromocriptine side effects
GI Orthostatic hypotension Headache Psychiatric disturbance Vasospasm Pulmonary infiltrates in high dosage
How to give Oxytocin?
IV
Oxytocin indications
Induction of labor
Control of uterine hemorrhage after delivery
Oxytocin side effects
Fetal distress Placental abruption Uterine rupture Fluid retention Hypotension
Oxytocin MOA
Mediates uterine contraction via activation of Oxytocin-R that are Gq coupled
Desmopressin MOA
Selective V2-R agonist
Synthetic analoge of ADH
Desmopressin indications
Central DI
Hemophilia A
Von-Willebrand disease
(increases insertion of water channels in CD in kidney; antiduiretic)
(extra-renal V2 receptors regulate release of cogulation factor 8 & von willebrand factor)
Desmopressin side effects
GI
Headache
Hypo-Natremia
Allergy
Rapid acting Insulin
Lispro
Aspart
glulisine
Lispro, aspart, glulisine Insulin
Onset of action
Peak
Duration
Onset of action: 10 min
Peak: 1 h
Duration: 3-4 h
Short acting Insulin
Regular Insulin
Regular Insulin
Onset of action
Peak
Duration
Onset of action: 30 min
Peak: 1-3 h
Duration: 4-8 h
Intermidiate acting Insulin
NPH (Isophan)
NPH (Isophan)
Onset of action
Peak
Duration
Onset of action: 1-2 h
Peak: 4-6 h
Duration: 8-12 h
Long Acting Insulin
gLArgine
detemir
degludec
Glargine
Onset of action
Peak
Duration
Onset of action: 2 h
Peak: Flat
Duration: 12-24 h
Rapid acting Insulin indications
Pre-parandial injection
contineous SC infusion devices
Emergency diabetic keto acidosis
Short acting Insulin indications
Pre-parandial injection (S.C)
Emergancy keto acidosis (iv)
hyperkalemia (iv)
Intermediate acting Insulin indications
Combined with short/rapid
Long acting Insulin indications
For Basal Insulin levels
What does human Inslin means?
Original AA sequence is not altered
What does analogue Inslin means?
AA sequence has been modified to generate more long/short acting Insulin
Insulin side effects
Hypoglycemia –> CNS
Injection site reaction
Edema
Total daily Insulin needs in T1DM
~ 0.55 Unit/Kg
Total daily Insulin needs in T2DM
> 1 Unit/Kg
GLP-1 analogue
Liraglutide
GLP-1 job?
Has the ability to decrease blood sugar levels in a glucose-dependent manner by enhancing the secretion of insulin
- its released from bowel in response to food.
- glucose-stimulated insulin release
- retard gastric emptying
- inhibit glucagon secretion
- feeling of satiety
GLP-1 and GIP are also called togather-
Incretins
Which GLP-1 drug can cause weight loss?
Liraglutide
Which DM patient will get Liraglutide
T2DM
What effect will a contineous Sulfonylurea use have?
Enhances tissue response to Insulin
Sulfonylurea 2nd generation
Glim.epi.rid
Glipi.zid
Which drug group is like Sulfonylurea MOA but is not a Sulfa drug?
Meglitinide
Meglitinides:
Rapeglinide
Sulfonylurea administration
Oral
Sulfonylurea side effects
Weight gain
Hypoglycemia
Skin Rash
Cardiovascular risk
Meglitinides side effects
Hypoglycemia
Meglitinides onset of action:
Meglitinides are more rapid than sulfonylurea
Biguanides MOA
- Activates AMPK –> Reduce hepatic & renal glucoNEO –> Post-parandial & fasting glucose level decrease
- Decrease intestinal glucose absorption
- Increase Insulin sensitivity
Metformin elimination
Renal
When does Metformin requires caution?
GFR < 45 mL/min/1.73 m2
Lower than 30 is contraindication
Metformin indications
it is a BIGuanide
- T2DM
- Restore fertility in anovulatory women with PCOS
- Weight reduction in obesity
- Hyperinsulinemia
Metformin side effects
GI
Lactic acidosis
Incertins actions
Increase Insulin release
Decrease Glucagon release
Delayed gastric emptying
Satiety
DDP-4 inhibitors
Vildagliptin
sitagliptin
DDP-4 inhibitors side effects
Headache Rhinitis nasopharyngitis (sitagliptin) Upper respiratory tract infections rare allergic rxn
SGLT2 location
Proximal convoluted tubule
When are SGLT2 inhibitors contraindicated?
Impaired renal function
SGLT2 inhibitors side effects
Genitourinary infections
Osmotic diuresis
a-glucosidase inhibitors
Acarbose
Acarbose side effects
Hypoglycemia
Diarrhea
Abdomianl pain
PTH effects in the kidneys
Decrease Ca2+ excretion
Increase Phosphate excretion
Vit. D synthesis
PTH effects in the bones
Osteoclast and blast activation
Net bone resorption in high conc.
Net bone formation in low conc.
PTH effects in the intestines
Ca2+ and Phosphate absorption mediated by Vit. D
PTH analogue
Teriparatide
How to give Teriparatide?
SC injection
Teriparatide indications
Osteoporosis
Teriparatide side effects
Hypercalcemia
Hypercalciuria
Vit. D3 is also called
Cholecalciferol
Cholecalciferol is given ____
Why?
Oral
Requires metabolism in liver (Calcifediol ) and kidney (calcitriol)to become the active form
Cholecalciferol indications
Vit. D def.
osteoporosis
osteomalacia
psoriasis
Cholecalciferol side effects
Hypercalcemia
Hyperphosphatemia
Hypercalciuria
What is the effect of Vit. D on PTH?
Vit. D inhibits PTH release
Calcitonin effects
- decreases serum calcium and phosphate by:
- inhibit bone resorption (Osteoclast activity)
- Kidney: Ca2+ and Phos. excretion
SERM used in Osteoporosis
Raloxifene
What is the effect of Estrogen on bones?
Inhibition of PTH-stimulated bone resorption
Raloxifene side effects
Hot flushes
Increased risk of thromboembolism
Bisphosphonates MOA
-Direct suppression of osteoclasts
(Inhibition of farnesyl
pyrophosphate synthase enzyme)
-inhibits bone resorption
- Rapid increase in bone mineral density in the first year
- Later equilibrium
Bisphosphonates:
Alendronate
Zoledronate
Alendronate
Zoledronate
Indications
Osteoporosis
Paget’s disease
Alendronate
Zoledronate
Side effects
- Hypocalcemia
- Adynamic bone
- gastric + esophageal irritation (patients should drink a lot of water)
- Osteonecrosis of the jaw (rare)
RANKL inhibitors
Denosumab
Denosumab
How to give and what is it?
SC injection every 6 months
IgG
Denosumab indications
Post menopausal osteoporosis
Denosumab side effects
Increase risk of infections
osteonecrosis of jaw (rare)