ADVANCE PHARMACOLOGY MIDTERM

ADVANCE PHARMACOLOGY MIDTERM

EXAM PRACTICE 2022 UPDATED

Routes of Administration - ANS-Patches, Suppositories, Sublingual tablets, Tablets, Liquid, Injectables, Sublingual, Nasogastric, Elixir (contains alcohol)

Parenteral Routes - ANS-intravenous, intramuscular, subcutaneous

Anti-diarrheals - ANS-Stops further occurrence of diarrhea. Notable medicines are Loperamide "Immodium" and Diphenoxylate with Atropine "Lomotil" Bismuth subsalicylate

Diphenoxylate HCl w/ Atropine Sulfate - ANS-The submucosal plexus controls the secretions of fluid and electrolytes in the lumen of the intestine. By acting on the presynaptic opioid receptors, it blocks the release of acetylcholine in the synaptic cleft and hence inhibits the motility and secretory action of the enteric nervous system.

Loperamide - ANS-acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel by binding to the opiate receptor in the gut wall

Bismuth Subsalicylate - ANS-The reduction in prostaglandin formation, as it inhibits cyclooxygenase. Prostaglandin induces inflammation and hypermotility. The stimulation of reabsorption of fluids, sodium, and chloride

Laxatives - ANS-Four main categories: Bulk, Stimulant, Osmotic, Stool Softener

enhancement of fluid retention by hydrophilic or osmotic mechanisms, decreasing net absorption of fluid through effects on the fluid and electrolyte transport in the small or large intestines, and finally an alteration of motility by inhibiting non propulsive contractions or stimulating propulsive contractions

Antiemetics - ANS-block serotonin from interacting with the 5-HT3 receptor. Of these, ondansetron and granisetron are the most frequently encountered. Intravenous (IV) and oral (PO) preparations are available. Side effects include headache, dizziness, and constipation Treats nausea and vomiting

Ulcers - ANS-Open sores in the lining of the digestive system

Drugs to treat ulcers - ANS-omeprazole (Prilosec), lansoprazole (Prevacid), rabeprazole (Aciphex), esomeprazole (Nexium) and pantoprazole (Protonix)

Irritable Bowel Syndrome - ANS-a common condition of unknown cause with symptoms that can include intermittent cramping, abdominal pain, bloating, constipation, and/or diarrhea

Drugs for Irritable Bowel Syndrome - ANS-Alosetron (Lotronex), Eluxadoline (Viberzi), Rifaximin (Xifaxan), Lubiprostone (Amitiza), Linaclotide (Linzess)

Alosetron (Lotronex) - ANS-works by blocking the action of serotonin on the intestinal system. This reduces the cramping abdominal pain, abdominal discomfort, urgency, and diarrhea caused by IBS

Eluxadoline (Viberzi) - ANS-contains mixed opioid receptors, including mu receptor agonist, a delta receptor antagonist, and a kappa receptor agonist. It acts locally in the enteric nervous system, and decreases adverse effects on the central nervous system.

Rifaximin (Xifaxan) - ANS-a semi-synthetic derivative of rifampin and acts by binding to the beta-subunit of bacterial DNA-dependent RNA polymerase blocking one of the steps in transcription. This results in inhibition of bacterial protein synthesis and consequently inhibits the growth of bacteria.

Lubiprostone (Amitiza) - ANS-selectively stimulates type 2 chloride channels in epithelial cells thereby causing an efflux of chloride into the intestinal lumen. The resultant fluid secretion into the gastrointestinal lumen provides a bolus effect that softens stool, increases intestinal transit, and improves symptoms of constipation

Linaclotide (Linzess) - ANS-contains an active ingredient called linaclotide, which reduces intestinal pain and accelerates gastrointestinal transit, according to nonclinical studies. The drug increases the cyclic guanosine monophosphate (cGMP) levels to decrease the pain

Crohn's and ulcerative colitis - ANS-NOD 2 upregulates receptor for muramyl (type of PAMP) (bacterial products) and increases nf-kb transcription which leads to a pro inflammatory state furthermore, absence or damage to tight junctions exacerbate inflammatory response.

Drugs for Crohn's and Ulcerative Colitis - ANS-Infliximab (Remicade), adalimumab (Humira) and golimumab (Simponi), Vedolizumab (Entyvio), Ustekinumab (Stelara)

Infliximab (Remicade) - ANS-neutralizes the biological activity of TNF-α by binding with high affinity to the soluble (free floating in the blood) and transmembrane (located on the outer membranes of T cells and similar immune cells) forms of TNF-α, and inhibits or prevents the effective binding of TNF-α with its receptors.

adalimumab (Humira) - ANS-a fully human IgG1 monoclonal antibody that specifically binds to tumor necrosis factor (TNF)-alpha, and is administered by subcutaneous injection. The mechanism of action is based on both the neutralization of TNF-alpha bioactivity and the induction of apoptosis of TNF-expressing mononuclear cells.

golimumab (Simponi) - ANS-a human monoclonal antibody that binds to both the soluble and transmembrane bioactive forms of human TNFa. This interaction prevents the binding of TNFa to its receptors, thereby inhibiting the biological activity of TNFa (a cytokine protein).

edolizumab (Entyvio) - ANS-contains humanised monoclonal antibody that works as antagonist to α4β7 integrin. The drug binds to α4β7 integrin, a mediator of gastrointestinal inflammation. Integrin receptors are proteins that function as mediators for cell-cell interactions.

Ustekinumab (Stelara) - ANS-binds to the p40 subunit of interleukin (IL)-12 and IL-23 and prevents their interaction with the cell surface IL-12Rβ1 receptor, subsequently inhibiting IL-12- and IL-23-mediated cell signaling, activation and cytokine production

Dextromethorphan - ANS--Antitussive (antagonizes NMDA glutamate receptors).-Synthetic codeine analog. Has mild opioid effect when used in excess.-Naloxone can be given for overdose. Mild abuse potential. -May cause serotonin syndrome if combined with other serotonergic agents

Loratadine - ANS-used to treat itching and redness caused by hives, it works by blocking the action of histamine, a substance in the body that causes allergic symptoms

Fexofenadine - ANS-selectively antagonize H1 receptors on the surface of cells on multiple different organ systems. It is a second-generation H1 receptor blocker and is non-sedating

Nasal Decongestants - ANS-Shrink mucosal membranes and reduces fluid secretion, should not be used for more than 48 hours oxymetazoline, phenylephrine, pseudoephedrine

Oxymetazoline - ANS-binds to and activates alpha-2 adrenergic receptors. Upon nasal or ocular administration, it constricts the arterioles in the nose and eye, resulting in decreased nasal and conjunctival congestion, respectively

Phenylephrine - ANS-an agonist of α1-adrenoceptors. Nasal decongestant action is mediated by activation of α1-adrenoceptors in the arterioles of the nasal mucosa. This causes vasoconstriction, which leads to decreased edema and increased drainage of the sinus cavities.

Pseudoephedrine - ANS-acts on α- and β2-adrenergic receptors, to cause vasoconstriction and relaxation of smooth muscle in the bronchi, respectively. α- Adrenergic receptors are located on the muscles lining the walls of blood vessels

Digoxin - ANS-Toxicity: Some early warning signs of overdose are confusion, loss of appetite, nausea, vomiting, diarrhea, or vision problems. Other signs of overdose are

changes in the rate or rhythm of the heartbeat (becoming irregular or slow), palpitations (feeling of pounding in the chest), or fainting Dosing: 0.125-0.25 mg orally/IV once/day; higher doses including 0.375-0.5 mg/day rarely needed.

Use: irregular heartbeats (arrhythmias) including atrial fibrillation

Statins - ANS-Atorvastatin, Rosuvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin and are recommended based on cardiovascular risk factors and LDL cholesterol levels/goals

Atorvastatin - ANS-competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG- CoA) reductase. By preventing the conversion of HMG-CoA to mevalonate, statin medications decrease cholesterol production in the liver

Rosuvastatin - ANS-works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body

Simvastatin - ANS-works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body

Pravastatin - ANS-The drug selectively acts on the rate-limiting step in cholesterol biosynthesis by inhibiting HMG Co-A reductase; this results in the upregulation of hepatic LDL (low-density lipoprotein) receptors enhancing LDL metabolism and clearance, which subsequently lowers the total plasma cholesterol in circulation

Lovastatin - ANS-class of medications called HMG CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body

Fluvastatin - ANS-It is prepared as a racemate of two erythro enantiomers of which the 3R,5S enantiomer exerts the pharmacologic effect. It selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase

Pitavastatin - ANS-completely inhibits HMG CoA reductase, the rate-determining enzyme in hepatic cholesterol synthesis. Consequently, LDL-C receptors in the liver are increased, thereby increasing the removal of LDL-C from the blood.

Colestipol - ANS-an oral cholesterol-lowering drug that is not absorbed from the intestine into the body. Rather, it works by binding to bile acids in the intestine and promoting the elimination of bile acids in the stool.

Nitroglycerin - ANS-denitrated by mALDH in smooth muscle and other cells. This results in the release of nitrite ion, which is then converted to nitric oxide. Nitric oxide that is