Drugs for GERD and Peptic ulcer , drugs for IBS and antiemetics Flashcards
Omeprazole
Pri-
Proton Pump Inhibitor (PPi) -prazole
ALL ARE PRODRUGS
MOA:
-Irriversible inhibits the H+/K+ATPase in the parietal cells –> so will prevent the exchange of H+ with K+ –> so no H+ in the lumen so no formation of HCl that is needed to convert pepsinogen to pepsin
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
Thera:
-First line for GERD –> reduces symtoms and heals erosive esophagitis
-H.pylori
-Can only use for 8 weeks
-Need to be taken 30min before breakfast and is daily use
Dose formulation:
DR Capsule: can sprinkle in apple sauce
Tablet: Do not crush do not spill
Packet: Mix with water
AE:
-Increase risk of upper respiratory tract infections
-Increase risk of osteoporosis –> because calcium and vitamin D need acid in the stomach in order to be absorb
Prilosec
Omeprazole + Sodium Bicarbonate
Zege
PPi -prazole
is a prodrug
MOA:
-Irriversible inhibit H+/K+ ATPase pump in the parietal cells
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
Thera:
-For gerd–> ppis have symptoms relief and healing of erosive esophagitis
-Can only use for 8 weeks and take it 30mins before breakfast
Formulations:
Capsule DR: open and sprinkle in apple sauce
Suspension: Only mix in water
AE:
-Increase risk of upper respiratory tract infections
-Increase risk of osteoporosis because calcium and vitamin D needs acid for absorption
Zegerid
Lansoprazole
Preva-
PPi (-prazole)
-Is a prodrug
MOA:
-Irriversible inhibits H+/K+ ATPase in the parietal cells –> so prevent the exchange of H+ with K+ in the lumen –> so no H+ in the lumen therefore no HCl that is needed to convert pepsinogen to pepsin
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
THERA:
-First line option for GERD –> it will reduce the symptoms and heal erosive esophagitis mucosa
-H.pylori
-Need to take it daily only for 8 weeks 30min before breakfast
Dosage forms:
-Capsule
-Tablet ODT
AE:
-Increase risk of upper respiratory tract infections because less acid so bacteria can grow
-Increase risk of osteoporosis –> because calcium and vitamin D need acid to be absorb
Prevacid
Pantoprazole
Proto
PPi (-prazole)
-Is a prodrug
MOA:
-Irriversible inhibits H+/K+ ATPase in the parietal cells –> so will prevent the exchange of H+ and K+ in the lumen –> so no H+ in the lumen therefore no HCl production that is needed to convert pepsinogen into pepsin
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
Thera:
-GERD–> is first line agent for gerd–> it will releif the symptoms and heals erosive mucosa
-H.pylori
-Can only take it for 8 weeks and on a empty stomach
Dosage forms:
-IV
-Tablet
-Packet –> dissolve in applesauce
-Suspension –> dissolve in applesauce
Protonix
Esomeprazole
Nex
PPI (-prazole):
is a prodrug
MOA:
-Irriversible inhibits H+/K+ ATPase in the parietal cells –> so prevent the exchange of H+ and K+ in the lumen –> so no H+ therefore no production of HCl that is needed to convert pepsinogen into pepsin
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
Thera:
-GERD–> relief symptoms and restore erosive esophagitis mucosa
-H.pylori
-Only for 8 weeks and need to be taken 30min before breakfast
Dosage forms:
-IV
-Tablet
-Cap
-Packet –> mix with water
AE:
-Increase risk of upper respiratory infections
-Osteoporosis –>because calcium and vitamin D need acid for absorption
Nexium
Dexlansoprazole
Kapi
PPI
MOA:
-Irriversible binds and inhibits the H+/K+ ATPase pump in the parietal cells so cause a more great reduction in acid formation
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
Thera:
-First line for GERD
-Can use for peptic ulcers
-Pt should take it 30 min before breakfast
AE:
-Increase risk of upper resp infections
-Increase risk of osteoporosis–> because Calcium and vitamin D need acid for absorption
Kapidex
Rabeprazole
aci-
PPI
MOA:
-irriversible binds and inhibits H+/K+ ATPase in the parietal cells
-Reduce acid formation much greater than H2RA
-Slow onset of action because they need to be absorb from the small intestine to the bloodstream and need to by pass the stomach. Because dont want them to get activated by the acid in the stomach so they are coated with sodium bicarbonate because the bicarbonate will neutralize the acid in the stomach so allows the PPI to pass the stomach without being activated and get absorb in the small intestine to the blood stream and then get to the parietal cells and irriversible bind and inhibits the H+/K+ATPase pump.
-Less risk of hypergrastemia because irriversible inhibits H+/K+ ATPase so the gastrin produce wont have a effect
-Less risk of the rebound acidity because irriversible inhibits the H+/K+ ATPase pump so the effects persist longer
Thera:
-First line for gerd
-Peptic ulcer
-H.Pylori
AE:
-increase risk of upper resp infections
-Increase risk of osteoporosis –> because calcium and vitamin D need acid for absorption
Aciphex
Cimetidine
H2RA (-tidine)
MOA:
-Reversible bind and blocks H2 Receptors on the parietal cells.
-They are faster onset of action because reversible binds and block so the effect will persist for less time. But not as effective on reducing acid secretion because:
-because gastrin can still be produce and bind to CCK-B receptors on the parietal cells some acid can still be produce
-Also ACH can still bind to M3 Receptors on the parietal cells and activate the H/K ATPase pump so some acid can still be produce
Thera:
-Second line for GERD
-For mild to moderate GERD
-Can take it with PPi
-Can take it on empty stomach
-For pt that have GERD and the symptoms are worse at night
PK: Peak 1-2hrs so short duration of action
Dosage forms: Tablet can crush tablet, solution, OTC, RX
Chronic use in H2RA can cause:
-Hypergrasteremia –> due to the low levels of acid the body will compensate by increasing secretion of gastrin so more acid will be produce
-Pt can also develop tolerance becase the body will increase the levels of acid due to less activation of H/K ATPase
AE:
-Vit B12 deficiency
-CNS effect if age is >50
-Cimetidine (Tagamate) can also block androgen receptors –> male can suffer from gynecomastia and decrease libido
DDi:
-Inhibits CYP 450
-Avoid in drugs that need acidic pH like azoles, protease inhibitors in HIV
Tagamet
Famotidine
H2RA (-tidine)
MOA:
-Reversible bind and blocks H2 R on the parietal cells –> so there is a reduction on acid secretion because less activation of the H/K ATPase pump
-But because gastrin can still be produced and bind to CCK-B receptors on the parietal cells and can still activate the H/KATPase pump so some acid is still produce
-Also ACH will bind to M3 receptors on the parietal cells and can cause some activation of H/KATPase pump
Thera:
-Second line for GERD
-For mild to moderate GERD
-Can take it with PPi
-Can take it on empty stomach
-For pt that have GERD and the symptoms are worse at night
PK: Peak 1-2hrs so short duration of action
Need renal dose adj
Dosage forms: Tablet, Suspension, IV
Chronic use of H2RA can cause:
-Hypergastremia –> due to the reduction in the levels of acid secretion the body will compensate by increasing the release of gastrin so more acid is produce
-Tolerance –> because the body will increase the levels of acid secretion due to the reduction in activation of the H/KATPase pump
AE:
-Vit B12 deficiency
-CNS effect if age is >50
DDi:
-Inhibits CYP 450
-Avoid in drugs that need acidic pH like azoles, rilpivirine in HIV
Pepcid
Nizetidine
Axi-
H2RA
MOA:
-Reversible binds and block H2 receptors so reduce the activation of H/K ATPase pump in the parietal cells
-So reduce the acid formation
-But because gastrin can still bind to CCK-B receptors on parietal cells and ACH to M3 receptors on parietal cells –> can activate the H/K ATPase so some acid can still be produce
-Faster onset
Thera:
-GERD
Chronic use of H2RA:
-Hypergastremia –> due to the reduction in acid secretion the body will compensate by increasing gastrin secretion so increases acid secretion
-Tolerance–> the reduction in acid secretion the body will compensate by increasing gastrin secretion so more acid secreted
AE:
-Increase risk of osteoporosis –> because calcium and vitamin D need acid for absorption
Axid
Sodium Bicarbonate
NaHCO3 –> NaCl + H2CO3 (Carbonic acid)
Antaacid
-For mild symptoms of GERD
-Fast onset of action
Dose: Hourly to PRN –> and if pt is using it very frequent consider a PPi
NaHCO3 is very water soluble and reacts fast
-The carbonic acid can decompose to H2O + CO2 –> and the CO2 can bind to the stomach lining of the stomach and cause bloating and increase production of HCl causing rebound acid
DDI:
-Drugs that require acidic pH like: Isoniazid, Ferrous Sulfate
-Tetracyclines and quinolones –> because chelation rxn can occur
Alkaseltzer
Calcium Carbonate
CaCO3
Antaacids
For mild symptoms of GERD
Quick onset of action
Dose: hourly or PRN –> if pt is using it frequently can consider a PPI
-CaCO3 is water insoluble, slow rxn –> but can cause constipation
DDI:
-Drugs that need acidic pH: isoniazid, protease inhibitors for HIV
-Quinolones and tetracyclines –> chelation rxn can occur
Tums
Magnisium Hydroxide
Mg(OH)2 –> MgCl + H2O
Antaacids
is water soluble but -Causes diarrhea
For mild symptoms of GERD
Quick onset of action
Dose: hourly and PRN –> if pt is using it very frequent consider a PPI
DDi:
-Drugs that require acidic pH–> isoniazid
-Quinolones and tetracyclines –> chelation rxn
Milk of magnesium
Alumminum Hydroxide
Al(OH)3 –> AlCl + H2O
ampho
Antiacids
Causes severe constipation
For pt with mild symptoms of GERD
Quick onset of action
Dose: hourly or PRN –> if frequent use –> consider a PPI
DDI:
Quinolones and tetracyclines
Drugs that require acidic pH
Amphogel
Magnesium Hydroxide + Aluminum Hydroxide
Antaacid
Reduces constipation and diarrhea but not 100%
Quick onset of action
Dose: hourly or PRN
For mild symptoms of GERD
Mylanta, Maalox
Sulcrafate
MOA:
-protect the lining of the stomach
-In the presence of acid sulcrafate will form a viscous polymer that will adhere to where the ulcer is like a band aid and will protect the ulcer from the acid
-Sulcrafate requires acid in order to form the viscous polymer so pt should avoid taking antaacids
Thera:
-For duodenum ulcer
Dose:
1gm PO QID
AE:
-Indigestion
-Constipation
-Dry mouth
DDI:
-Sulcrafate can interfere with the absorption of other drugs so pt space out the other drugs
-Digoxin
-Warfarin
-Quinolones
-Antifungals
Carafate
Misoprostol
Cyclo
PGE2 receptor agonist
MOA:
-It will bind to PGE2 receptors on the GIT lining and will increase production of mucus and bicarbonate
Mucus–> provide protection
Bicarbonate–> neutralize the acid environment
Thera:
-only for ulcers
AE:
-Increase contraction of the uterus by causing increase blood flow –> induce labor
-Severe diarrhea
CI:
-Pregnant
Cytotec
Voroprazan
Vorq
Potassium Competitive acid Blocker (PCAB)
MOA:
-Binds to where Potassium binds in the H/K ATPase pump and reversible inhibits the H/KATPase pump
Because is reversible bound –> pt can suffer from hypergrastemia and if pt suddenly stops can also suffer from acid rebound
Vorquenza
Lubiprostone
ami-
Lubiprostone (amitiza)
ClC2 activator
MOA:
-directly activates ClC2 co transporter in the GIT cells so Cl- moves out from the cell into the lumen and draws H2O in into the lumen
So treat IBS-C - constipation
AE:
-Diarrhea because more H2O in
Linaclotide
Linzi-
Linaclotide (Linziness)
Uroguanylin receptor agonist
MOA:
-Linaclotide (Linziness) will bind and activate uroguanylin receptors on cells that line the GI and is a guanylate cyclase receptor –> so activation of a guanylate cyclase receptor will lead to convert GTP ->to cGMP –> cGMP will activate protein kinase G –> protein kinase G will phosphorylate Cl co transporters –> so Cl move out from the cell into the lumen and draws H2O into the lumen –> so treat IBS-C –> constipation
Counsel:
-Linaclotide (linziness) is a peptide so pt need to take it on a empty stomach because if it take it with food it will activate the acid secretion in stomach and will breakdown linaclotide
Plecanatide
tru-
Plecanatide (Trulance)
Uroguanylin receptor agonist
MOA:
will bind and activate uroguanylin receptors on cells that line the GI and is a guanylate cyclase receptor –> so activation of a guanylate cyclase receptor will lead to convert GTP ->to cGMP –> cGMP will activate protein kinase G –> protein kinase G will phosphorylate Cl co transporters –> so Cl move out from the cell into the lumen and draws H2O into the lumen –> so treat IBS-C –> constipation
Prucalopride
Mote-
Prucalopride (motegrity)
Selective 5HT4 receptor agonist
MOA:
-Activate 5HT4 receptor in the GIT –> so increase contraction and motility of GIT –> treat IBS-C
Tegaserod
Tegaserod (Zelnorm)
Partia 5HT-4 receptor agonist but has poor selectivity
-Activates 5HT 4 in the GIT –> increase contraction and motility of GIT –> treat IBS-C
But can activate 5HT1B –> in blood vessel –> causes constriction of blood vessels and coronary artery –> increase risk of MI and stoke
-Can also activate 5HT1D
AE:
-Increase risk of MI and stroke
CI:
-pt with angina, MI, stroke
Tenapanor
Tenapanor (Ibsenra)
NHE antagonist
MOA:
-Block NHE (Na- H+ exchanger) in the GIT so Na+ stays in the lumen and H2O will follow Na+ so H2O stays in the lumen –> treat IBS-C constipation
AE:
-Diarrhea
