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Model Drug List -Exam 3

Terms in this set (36)

Epinephrine
Non-selective beta-2 adrenergic agonist that is considered the most effective bronchodilator. It also has some alpha adrenergic effects, including bronchoconstriction (outcompeted by beta-2 bronchodilation effects in respiratory tract), vasoconstriction, and decreased airway congestion, which is why it is rarely used outside of emergency situations (i.e. anaphylactic shock and other histamine related effects)
Diphenhydramine
First generation H1 antagonist (antihistamine) that competes with histamine for receptors but does not prevent release of histamine, allowing it to still affect serotonin and the arachidonic acid cascade. Due to being able to cross the blood-brain barrier, it has CNS side effects like sedation and drowsiness, as well as some anticholinergic effects.
Maropitant
Neurokinin-1 receptor antagonist that has both central and peripheral antitussive effects, thus making it a highly successful non-narcotic centrally-active antitussive drug. Additionally, by blocking these receptors, it blocks the effects of substance P, the main mediator of the vomiting center, leading to antiemetic effects.
Cyclophosphamide
Alkylating agent prodrug that functions by alkylating DNA in bone marrow cells, leading to DNA damage. This is especially debilitating to B cells, since they take longer to recover than T cells, and suppressed the body's ability to produce antibodies. Since it targets all bone marrow cells, it can lead to bone marrow suppression, which can lead to secondary infections, thrombocytopenia, and anemia. It may also cause sterile hemorrhagic cystitis, or bleeding of the urinary bladder mucosa.
Azathioprine
Antimetabolite purine analog prodrug that targets bone marrow and inhibits DNA synthesis. It is indicated in severe autoimmune diseases or in patients that are non-responsive to glucocorticoid treatment. It is generally considered safer than alkylating agents due to having fewer side effects, but it still may cause hepatotoxicity or leuko/thrombocytopenia.
Cyclosporine
Calcineurin inhibitor that is particularly good at inhibiting T cells. Calcineurin is a calcium and calmodulin dependent phosphates that produces, among other things, IL-2, which is important in T cell activation, and this is suppressed by this drug. Because this drug does not target DNA directly, only transcription factors, it does not suppress non-specific immunity nor does it cause myelosuppression. It is highly lipophilic so it must be prepared as an oil solution. It is broken down into 25-30 metabolites, contributing to highly variable pharmacokinetics and drug interactions.
Oclactinib
Tyrosine kinase inhibitor that preferentially targets JAK-1 and JAK-2 ("just another kinase"), which primarily signal for IL-31, which in turn signals for pruritis and allergies. This drug is approved for use in dogs with atopy associated pruritis.
Loratidine
Second generation H1 antagonist (antihistamine). These drugs are less lipophilic than first generation H1 antagonists and they bind preferentially to peripheral receptors rather than CNS receptors, so they do not have as many CNS side effects as the first generation. They have anti-allergy properties so they are used to treat acute inflammation and allergic reactions.
Cyproheptadine
Antiserotonergic antihistamine (serotonin antagonist). Because serotonin contributes to the acute stages of the asthma response by mast cell degranulation, it can be used in cats to counteract this response. It also affects serotonin receptors in the hypothalamus, so it can also be used to stimulate appetite in cats.
Famotidine
H2 receptor antagonist that competitively and reversibly blocks the H2 receptors in the parietal cells of the stomach, causing a disturbance in the cAMP-dependent pathway, which in turn shuts down the H+/K+ATPase. This will prevent acid from being pumped into the gastric lumen, raising pH and protecting the epithelium. This particular drug is 32 times more potent than the first generation H2 receptor antagonist (cimetidine), is not effective for treating NSAID induced ulcers, and generally has fewer side effects than cimetidine.
Omeprazole
Proton pump inhibitor that functions by irreversibly blocking the H+/K+ATPase, preventing acid from being pumped into the gastric lumen. This drug's efficacy is characterized by a long latent period due to new channels being formed to replace the blocked ones. However, it also has a slow onset due to being a weak base and getting trapped by protons in the acidic parietal cells. It is 30 times more potent than cimetidine.
Misoprostol
Prostaglandin E1 analog that activates EP3 channels by mimicking the actions of PGE1, which suppresses the cAMP pathway, which shows acid production. It increases bicarbonate and mucus secretions, and it also increases mucosa blood flow and epithelial cell growth. Because of this action, this makes it one of the more effective drugs for preventing NSAID associated ulcers. It may also cause abortions, so it should not be used around pregnant women.
Sulcrafate
Cytoprotective agent that functions by dissociating into sucrose octasulfate and aluminum sulfate, the former of which is a sticky, viscous substance that binds to ulcerated mucosa and protects it from the acidic environment, giving it a chance to heal. It needs the acidic environment to disassociate so it cannot be given with antacids. The aluminum sulfate metabolite can also bind to other drugs so it should not be given in conjunction with other orally available drugs.
Mirtazipine
Indirect appetite stimulant that was originally used as a human antidepressant. It's method of action is antagonism of 5-H7-2c, which is a serotonin receptor and under normal conditions would be an appetite suppressant. This drug also can have antiemetic and antinausea effects.
Capromorelin
Hunger center agonist that selects for ghrelin receptors. Ghrelin is normally secreted by the stomach to stimulate appetite, weight gain, and an increase in serum growth hormone levels. As an agonist, this drug has similar effects.
Apomorphine
Centrally acting emetic agent that is a morphine derivative, but it does not have opiate effects. Instead, it acts as a non-specific dopamine receptor agonist, inducing emesis by stimulating the chemo-receptor trigger zone (CRTZ) of the central nervous system. It is contraindicated in cats as it causes too much excitement.
Ropinirole
Centrally acting emetic agent that acts as a dopamine-2 agonist. It is commonly given as a topic ophthalmic agent (in the eye).
Metoclopramide
Dopamine antagonist that acts centrally on the dopamine receptors in the chemo-receptor trigger zone (CRTZ). It also can inhibit serotonin receptors at high doses and can cross the blood-brain barrier to inhibit the receptors at the vomiting center. It has additional kinetic effects that works to move potential vomitus from the stomach and duodenum into the lower GI tract. It does have some effects like sedation due to it being a broad spectrum antagonist.
Ondansetron
Serotonin antagonist antiemetic that is highly selective for the 5-HT3 receptor. By inhibiting this receptor, it prevents serotonin from signaling for vomiting, as well as limiting serotonin's effects on the entire GI tract.
Meclizine
H1 receptor antagonist. As it is an antihistamine, is most useful as a motion sickness drug, as it blocks histaminergic emesis.
Psyllium (seed)
Prebiotic dietary fiber that stimulates the growth of resident gastrointestinal bacteria in the colon, as they are able to ferment this fiber. The seeds are also used as a simple bulk laxative, causing the fecal matter in the colon to absorb water and swell. This results in colonic distention, causing reflex contraction, and finally leading to peristaltic activity.
Kaolin-Pectin
Two drugs that are almost always given in tandem as both adsorbants and protectants. They function by binding to bacteria and bacterial products (i.e. toxins) to reduce inflammation. They do no reduce the loss of fluid or electrolytes, so they are only effective for mild to moderate diarrhea, not severe.
Bismuth Subsalicylate (Pepto-Bismol)
Antisecretory protectant that is used as an acute diarrheal treatment and has two modes of action:
1. Bismuth provides antisecretory and gastrointestinal protective effects
2. Subsalicylate inhibits inflammatory prostaglandins, lowering gastrointestinal secretions and modulating gastrointestinal motility
Mineral Oil
Emollient (a.k.a. stool softener) that acts by directly lubricating feces, which facilitates expulsion. As an emollient, by definition, it is not digested (as opposed to simple bulk laxatives, which are digested).
Magnesium Hydroxide (Milk of Magnesia)
Hyperosmotic cathartic, meaning it functions by attracting water into the intestinal lumen by increasing osmotic forces, preventing reabsorption. This particular drug releases Mg+ ions in the GI tract, which causes an increase in CCK, leading to increased peristaltic activity.
Lactulose
Hyperosmotic cathartic, meaning it functions by attracting water into the intestinal lumen by increasing osmotic forces, preventing reabsorption. This particular drug is a synthetic disaccharide that is metabolized by colonic bacteria, creating organic acids. These acids help to prevent colonic absorption of metabolically produced ammonia, so it is useful in patients with hepatic disease, because they cannot properly process ammonia.
Ursodeoxycholic Acid (Ursodiol, UDCA)
Anticholestatic endogenous bile salt of bears that protects cholangiocytes against the cytotoxicity of bile acid, stimulates hepatobiliary secretions, and protects against bile acid-induced apoptosis. It is used to treat primary biliary cirrhosis, cholestatic liver disorder, and chronic liver disease.
S-adenosyl-L-methionine (SAMe)
Hepatoprotective agent that is an endogenous compound of the liver that is important in 3 major metabolic pathways:
1. Transmethylation
2. Aminopropylation
3. Transsulfuration
The last of these processes is needed for the production of glutathione, a scavenger of oxygen radicals in cells, which is produced in the liver. As a drug, it is a nutritional supplement given to patients with hepatic disease or as an adjunctive therapy to patients receiving potentially hepatotoxic drugs, like acetaminophen.
Thyroxine (T4)
Thyroid hormone that is protein bound in the blood until it is taken up by the cells and converted to its active form. It is the result of thyroglobulin being iodized by the thyroid peroxidase, creating mono- and di-iodinated tyrosine. This hormone is the product of two di-iodinated tyrosines, while the active form (triiodothyronine) is the product of a mono- and a di-iodinated tyrosine. This hormone is given as a supplement for hypothyroidism.
Methimazole
Thyroid hormone antagonist that inhibits the formation of T3 and T4 by being preferentially iodinated by the thyroid peroxidases. It is a pharmaceutical option for treating hyperthyroidism.
Calcitrol
Active form of Vitamin D, such that it does not have to undergo renal or hepatic metabolism, and can therefore begin meditating parathyroid hormone responses immediately. Due to its mechanism, improper use may lead to hypercalcemia, so it should be given with caution. Because there are other options that are less potent, and therefore safer, it is mainly indicated in chronic renal failure related hypoparathyroidism, since the kidneys do not have to process this supplement.
Cholecalciferol
Form of Vitamin D that must undergo both renal and hepatic activation before it can begin meditating parathyroid hormone responses. Because these responses control the levels of calcium in the body, it may also need to be given with calcium supplement to have a noticeable effect.
Regular Insulin
Pancreatic hormone that facilitates glucose uptake into cells. It is produced in the β pancreatic cells and is a protein hormone, so it must be given parenternally. This particular form of this hormone has the quickest onset, but also the shortest duration, so its use is typically reserved for life threatening situations like diabetic ketoacidosis. It is the only type of this hormone that can be given IV, but, due to the nature of this hormone, it will bind to plastic particles in the IV line, so the line must be flushed before administering the drug to patients.
Protamine Zinc Insulin
Pancreatic hormone that facilitates glucose uptake into cells. It is produced by adding protamine or zinc to the endogenous form of this hormone and is a protein hormone, so it must be given parenternally. This particular form of this hormone has a relatively slower onset and is longer acting than the endogenous form, so it is labeled as the intermediate form.
Glargine Insulin
Pancreatic hormone that facilitates glucose uptake into cells. It is produced by substituting an amino acid from the endogenous form of this hormone and is a protein hormone, so it must be given parenternally. This particular form of this hormone has one of the longest durations of action (up to 24 hours), so it is considered long acting.
Detemir Insulin
Pancreatic hormone that facilitates glucose uptake into cells. It is produced by adding a lipid to the endogenous form of this hormone and is a protein hormone, so it must be given parenternally. This particular form of this hormone has the one of the longest durations of action (up to 24 hours), so it is considered long acting.
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