GI drugs Flashcards by SamanthaJoan90 .

what is the area is the area that receives vomiting relays?

nucleus tractus soltarius

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What are the 3 areas that relay information to the nucleus tractus solitarius?

GI tract
vestibular system
area postrema

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How does the GI tract trigger emesis?

stomach release 5HT3 that bin to vagal efferents that cause emesis

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how does the vestibular system cause emesis?

CN VIII communicates with NTS–> emesis

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How does the area postrema cause emesis?

its located to the NTS outside the BBB in the 4th ventricle ;responds to emtogenic substances

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Ondanseton

antagonizes 5HT 3 receptors on the vagal afferent of GI tract

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What are the side effects of ondansetron?

constipation 
headache
dizziness 
QT prolongation--> torsade de pointes 
serotonin syndrome

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What are the receptors located in the vestibular system ?

H1 receptors

and Muscarinic receptors

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Antihistamines & scopolamine

tx: motion sickness

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What are the side effects of antihistamines

antimuscarinc
sedation
mydriasis

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What is the receptor in the area postrema ?

D2 receptors

NK 1 receptors

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Metochlopramide

antagonize D2 receptors in area postrema

pro kinetics –> increased gastric emptying

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What are the side effects of metochlopramide?

contraindicated in small bowel obstruction 
diarrhea
drowsiness 
depression 
extrapyramidal effects 
Tar dive dyskinesia 
Neuroleptic malignant syndrome 
increase prolactin levels 
torsade de pointes

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What activated NK1 receptors in area postrema?

substance P

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Aprepitant

antagonizes NK1 receptors in area postrema

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Ranitidine, Cimetidine, famotidine

H2 antagonist
“tidine”
tx: GERD
gastric & duodenal ulcers

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Omeprazole, lanoprazole

"prazole"
proton pump inhibitors 
tx:GERD
NSAID induced ulcers
H.pylori 
Gastrinomas

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What are the side effects of proton pump inhibitors

increased clostridium difficile 
increase osteoporosis
increased respiratory infections 
decreased Ca,Fe, Mg, absorption 
hypomagnesium

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Octreotide

Somatostain anolog
inhibit G cells from releasing gastrin
decrease release of histamine by ECL cells

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Rifaximin

decrease the ammonia produce by intestinal bacteria

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Psyllium

gulf forming laxative

Decussate , Enema

stool softners

Senna

stimulates laxative

can cause melanosis coli

loperamide , diphenoxylate

active mu receptors decrease bowel movements

What type of cancers can octreotide be given for?

VIPoma | carcinoid tumors

Gluisine, Aspart, lispro

short acting | tx; post prandial meals

Regular insulin, NPH insulin

intermediate acting given IV tx: diabetic ketoacidosis hyperkalemia

Detemir, Glargine

allows for steady level of insulin | can cause hypoglycaemia

Tolbutamine , chlorpropamide

1st generation sulfonylureas | bind to ATP dependent K channels--> depolarization--> ca influx --> insulin release

glyburide, glimepriride, glipizide

2nd generation sulfonylureas | glipizide is short acting

ropaglinide, nateglinide

''glide" bind K channels no sulfa interaction

What is the side effects of sulfonylureas and glinides?

increased risk of hypoglycaemia increase weight gain disulfram reaction with alcohol

eventide, liraglutide

act on GLP-1 receptors | increase insulin , decrease glucagon, decrease gastric emptying-- satiety

Sitagliptin, saxagliptin, linagliptin

"gliptin" | prevent the breakdown of GLP-1

What are the side effects of DDP4

nasopharyngitis | upper respiratory infections

Metformin

inhibit mitochondrial enzyme glycerophosphate dehydrogenase--> decrease hepatic gluconogenesis activates AMPK--> decreases gluconeogenesis

What is the side effects of metformin

``` lactic acidosis contraindicated with renal insufficiency GI effects (anorexia, vomiting) ```

Rosiglitazone, Pioglitazone

increase glucose use is a ligand of PPAR-gamma --> unregulated adiponectin increased adipocytes --> decreased TGs unregulated glut 4

What are the side effects of thiazolidinediones

fluid retention & peripheral edema weight gain exacerbate HF decrease bone mineralization --> fractures

Amylin

decrease glucagon , gastric emptying & appetite tx : type 1 &2 hypoglycaemia

Acarbose & miglotol

Alpha glucosidase inhibitor decrease conversion of disaccharides to absorbable monosaccharides located in brush border

What are the side effects of alpha glucosidase inhibitors

diarrhea, flatulence, abdominal pain

Canagloflozin, dapagloflozin

SGLT2 inhibitors | decrease reabsorption of glucose in PCT

What are the side effects of SGLT2 inhibitors

increase UTI due to glucose concentration in urine candidiasis (genital) hypotension contraindicated in renal insufficiency

Alendronate, pamidronate, zoledronate

1st line tx attach to hydroxyapatite in bone --> osteoclast binding to bisphosphonates instead of bone --> decrease activity induce osteoclast apoptosis decrease the development & recruitment of osteoclast precursors tx; hypercalcemia, hypercalcemia malignancy paget disease

What are the effects of bisphosphonates

``` GI effects esophagitis esophageal ulcers acid reflux osteonecrosis of the jaw hypocalcemia increase risk of breast cancer taken with a lot of water ```

What is the effects of estrogen on bone?

inhibit differentiation of osteoclast precursors

Raloxifene

SERM agonist in bone: antagonist in breast and uterus tx; prevention of postmenopausal osteoporosis

What is the action of PTH on bone ?

stimulates osteoblast to express RANKL RANKL binds to RANK to increase osteoclast activity

Denosumab

directly inhibit osteoclast promote Ca excretion from the kidney tx: paget hypercalcemia of malignancy