Term
| What was the first ever chemical compound isolated from plants? |
|
Definition
|
|
Term
|
Definition
| Opium poppy (species name) |
|
|
Term
| Opium poppy is an _______ grower. |
|
Definition
|
|
Term
| What part of opium poppy is extracted to make drugs? Where can this be found in the plant and what is the primary source of extraction? |
|
Definition
- The alkaloid rich latex is extracted to make drugs
- The alkaloids are found in all tissues but are primarily extracted from the capsule fruit of opium poppy |
|
|
Term
| True/False: The opium poppy plant is not native to the U.S. but is grown here. |
|
Definition
|
|
Term
| What are some uses of poppy? |
|
Definition
| Poppy seed oil, food, drugs, teas, etc |
|
|
Term
| How was heroin originally introduced and for what? |
|
Definition
| Heroin was introduced by Bayer as a "non-addictive" substitute for morphine/ cough medicine. However it was 6x more addictive and was taken off the market after 20 years. |
|
|
Term
| What country is the world leader in opium supply and who controls these fields? |
|
Definition
|
|
Term
| Where does the U.S. get most of it's opium from? |
|
Definition
|
|
Term
| What is the difference between opiates and opioids? |
|
Definition
| Opiates are the compounds naturally produced by the plant (alkaloids). Opioids are compounds that act like opiates and bind to opioid receptors in the body ( includes opiates, semi-synthetic + synthetic drugs, endogenous opioids) |
|
|
Term
| What alkaloid of opium poppy is used to treat smooth muscle spasms? |
|
Definition
|
|
Term
| What opium poppy alkaloid is used to synthesize oxycodone (an analgesic)? |
|
Definition
|
|
Term
| What is the strongest/most addictive opium poppy alkaloid? |
|
Definition
|
|
Term
| What alkaloid is used as an alternative to morphine because it was less addictive? |
|
Definition
|
|
Term
| True/False: Prescription opioid use is less prevalent now than it was 20 years ago. |
|
Definition
| False. We use opioids more often now. |
|
|
Term
| Are men or women more likely to use opioids? |
|
Definition
| Women- and mostly people above 40. |
|
|
Term
| How do we collect the alkaloid-rich latex from the poppy fruits? |
|
Definition
| The fruits are scored when they are still immature and the latex weeps out and is later collected. |
|
|
Term
| What amino acid is used to start morphine biosynthesis and where does it come from? |
|
Definition
| The process begins with Tyrosine, which is produced during photosynthesis. |
|
|
Term
| Describe the process of morphine biosynthesis. |
|
Definition
- Begins with Tyrosine, goes through enzymatic reactions
- Produce Reticuline, goes through enzymatic reactions
- Produces morphinone and codeinone which then produce the final product of morphine |
|
|
Term
| What two alkaloids are produced from Tyrosine? |
|
Definition
|
|
Term
| Locally within the opium poppy plant where does morphine biosynthesis take place? |
|
Definition
| It begins in the sieve elements (floem) and then most is transferred into the laticifers (cells that produce latex) and stored. |
|
|
Term
| What alkaloid is morphine made from? What other way can morphine be produced? |
|
Definition
-Codeine
-Morphine doesn't have to be made via the Tyrosine pathway. it can be produced from thebaine -> oripayine -> morphinone-> morphine |
|
|
Term
| What is morphine's mechanism of action? What does this mean? |
|
Definition
| Morphine is an agonist, meaning it binds directly to receptors, activates them, and causes response. |
|
|
Term
| Where in the body are opioid receptors located? |
|
Definition
| CNS- brain, brain stem, spinal cord |
|
|
Term
| What are the three types of known opioid receptors? Which is most important? |
|
Definition
- Mu, Kappa, Delta
-Mu is most important |
|
|
Term
| What are effects of the opioid receptors being activated? |
|
Definition
| Analgesia, respiratory depression, euphoria, sedation, constipation, anxiety, physical dependence |
|
|
Term
| Which opioid receptor is morphine most active at? What about codeine and hydromorphone? |
|
Definition
| All are most active at Mu |
|
|
Term
| Codeine only binds at _____ receptors. |
|
Definition
|
|
Term
| Where specifically are Mu receptors located? What is their effect? |
|
Definition
Membrane of neuronal cells
They affect the reward/pain system |
|
|
Term
| What are the four main actions of morphine? |
|
Definition
| Sedation (coma at high doses), euphoria (main reason for abuse), analgesia, and respiratory depression (apnea) |
|
|
Term
| How does morphine (and heroin) lead to a release of dopamine? What is dopamine associated with? |
|
Definition
- Morphine binds to Mu and blocks release for GABA receptors, leading to a release of dopamine
-Dopamine is associated with reward/motivation |
|
|
Term
| Who does morphine act as an analgesic? |
|
Definition
| Morphine reduces the activity of nociceptors, or sensory nerves that respond to damaging stimuli by sending signals to the CNS. When nociceptors can't send signals to the brain, we don't feel the pain. |
|
|
Term
| What prescription forms of morphine are available? |
|
Definition
| Injectable, oral, immediate and controlled release tablets, suppositories |
|
|
Term
| What drug class is Morphine? What prescription forms are available? |
|
Definition
Narcotic analgesic (schedule II)
Injectable, oral solution, immediate release tabs, controlled release tabs, suppositories |
|
|
Term
| What is methadone used for? |
|
Definition
| It is used to ween people off of drugs such as heroin because it doesn't have as many severe side effects. |
|
|
Term
| What is the difference between the oral availability, half life, and duration of action in morphine and methadone? |
|
Definition
| Morphine has a much smaller bioavailability. It also has a much shorter duration of action and half life. |
|
|
Term
| What is the difference, for example, between nasal entry of morphine versus oral admin? |
|
Definition
| Morphine given nasally goes directly to the brain. Given orally is must pass through intestinal track and make its way to the brain so much of it is broken down into other compounds. |
|
|
Term
| What are some side effects of morphine? |
|
Definition
| Physical dependence, tolerance, respiratory depression, sedation, cognitive impairments, gastrointestinal effects, histamine effects |
|
|
Term
| What is the treatment for opioid acute intoxication? |
|
Definition
| Treatment is to decrease mortality (chance of death). Usually give Naloxone, an antagonist which prevents further opioids from binding. |
|
|
Term
| What are the functions of the GI tract? |
|
Definition
| Digestion, secretion (enzymes, saliva, etc), absorption, motility |
|
|
Term
| What are the three sections of the GI tract? |
|
Definition
|
|
Term
| What organs comprise the foregut? |
|
Definition
| Pharynx, esophagus, stomach, and small intestine |
|
|
Term
| The small intestine and large intestine are both a part of which section of gut? |
|
Definition
|
|
Term
| The hindgut is comprised of? |
|
Definition
| Large intestine, rectum, and anus |
|
|
Term
| Where does the bulk of digestion occur? What else occurs here? |
|
Definition
| In the small intestine and it also performs a lot of absorption |
|
|
Term
| The stomach does not so much perform digestion, but rather is responsible for________. |
|
Definition
|
|
Term
| What does GERD stand for? PUD? |
|
Definition
Gastroesophageal Reflux Disease
Peptic Ulcer Disease |
|
|
Term
| What is the function of the lower esophageal sphincter (LES) and what is its role in GERD? |
|
Definition
| The LES prevents acid and pepsin from coming up and into the esophagus. Decreased tone of the LES leads to GERD. |
|
|
Term
| What are the acute symptoms of GERD? |
|
Definition
| Heart burn (chest pain) and regurgitation when lying down |
|
|
Term
| What are some symptoms of chronic GERD and what is most concerning about this? |
|
Definition
Cough, shortness of breath, esophageal ulceration and stricture, Barrett esophagus (change in epithelium to match stomach)
There is a MAJOR risk for cancer, particularly with Barrett esophagus (adenocarcinoma) |
|
|
Term
| What are the four methods of treatment for GERD? |
|
Definition
All are acid suppressors:
-Histamine (H2) Antagonists
-Proton pump inhibitor (PPI)
-Prostaglandin analogs
-Muscarinic antagonists |
|
|
Term
| What is the earliest historic reference to cancer and where does the name come from? |
|
Definition
| The earliest references date back to ancient Egypt with cases treated by cautery. The name "cancer", meaning crab, was described by Hippocrates because of its invasive projections. |
|
|
Term
| What is the second leading cause of death in the US? |
|
Definition
|
|
Term
| What percentage of the US population is diagnosed with cancer? What is the deadliest form of cancer? |
|
Definition
| Over 25% of population is diagnosed with cancer during their lifetime. Lung cancer is the most deadly form. |
|
|
Term
| What are some cellular hallmarks of cancer? |
|
Definition
-Growth without control (proliferation due to loss of tight control on cellular growth)
-Evasion of apoptosis
-Sustained angiogenesis (continued blood supply)
-Tissue invasion and metastasis
-Self sufficiency in growth signals and insensitivity to anti-growth signals |
|
|
Term
| Who is the Father of Chemotherapy and how was it discovered? |
|
Definition
Farber- Was experimenting with drug that interfered with folic acid metabolism necessary for DNA replication.
During WWII, mustard gas was developed and found to work against lymphoma. It damages the DNA of cancer cells. |
|
|
Term
| The mammalian CV system is _______ and the lymphatic system is ______. |
|
Definition
|
|
Term
| Explain how blood pressure (P=QR) works. |
|
Definition
P is equivalent to blood pressure.
P equals the resistance of blood to the the lumen diameter( R) x the flow of blood through the lumen (Q). |
|
|
Term
| Blood pressure is an analog of ______. |
|
Definition
|
|
Term
| MAP stands for___________ and is equivalent to? |
|
Definition
Mean arterial pressure
It is equivalent to blood pressure, systolic over diastolic |
|
|
Term
|
Definition
| Cardiac output = stroke volume x heart rate |
|
|
Term
| What is the clinical term for high blood pressure? |
|
Definition
|
|
Term
| What action of morphine is directly related with mu receptor agonism? |
|
Definition
|
|
Term
| What may be given to help with opioid withdrawal? |
|
Definition
| Methadone, buprenorphine, clonidine to help with detox |
|
|
Term
| What are two methods of treating opioid addiction? |
|
Definition
| Total abstinence oriented or opioid agonist maintenance |
|
|
Term
Match the receptor (Mu, Kappa, Delta) with its effects:
1. Tolerance, anxiety, depression
2.Analgesia, respiratory depression, euphoria, sedation, constipation, dependence
3. Analgesia, respiratory depression, sedation, dependence, anxiety, depression |
|
Definition
|
|
Term
| Drugs ending in -tidine are a part of what drug group? |
|
Definition
|
|
Term
| Describe the mechanism of action for Histamine (H2) Receptor antagonists? |
|
Definition
| Reversible H2 antagonist -> decrease in cyclic AMP -> decrease in proton pump activity |
|
|
Term
| What group does the drug Cimetidine belong to? What does it treat? What are some other drugs that belong to the same group? |
|
Definition
Histamine Receptor Antagonists
Prescribed for GERD, PUD
Famotidine, etc. |
|
|
Term
| Drugs ending in -prazole belong to what drug group and treat? |
|
Definition
Proton Pump Inhibitors( PPIs)
Treatment for PUD, GERD (even severe), gastritis |
|
|
Term
| What drug group is Omeprazole a part of? What is this groups MOA? |
|
Definition
PPIs
They cause irreversible H+/K+ proton pump inhibition on gastric parietal cells |
|
|
Term
| What is rebound gastric acidosis? |
|
Definition
| When a patient stops use of a PPI (for example), the body rebounds by producing tons of acid and the issue can be worse than before |
|
|
Term
| What are some potential side effects of PPIs? |
|
Definition
| Parietal cell hyperplasia, rebound gastric acidosis, pneumonia, hip fracture, increased risk for Clostridium difficile |
|
|
Term
| What group of people is Misoprostol contraindicated for? Why? |
|
Definition
| Pregnant women because it is an abortifacient, inducing labor/miscarriage |
|
|
Term
| What is typically prescribed for NSAID-induced PUD? |
|
Definition
| Prostaglandin analogs, like Misoprostol |
|
|
Term
| What is the MOA for muscarinic antagonists? What is one example of this drug type? |
|
Definition
They decrease Ca2+ in gastric parietal cells.
Atropine |
|
|
Term
| What are the effects of muscarinic antagonists? |
|
Definition
| Dry mouth, dry eyes, constipation, etc. due to their anti-muscarinic effects |
|
|
Term
| Why are muscarinic antagonists not used very often? |
|
Definition
| Their are superior drugs with fewer side effects available. |
|
|
Term
| Calcium carbonate is what kind of drug? What is the more common name? |
|
Definition
|
|
Term
| What is the MOA for antacids? |
|
Definition
| They neutralize stomach acid which is already present. Only temporary/mild relief. |
|
|
Term
| What are some issues with continued antacid use? Explain. |
|
Definition
1. Hypokalemia (low K+)- When we use antacids to lower our bodily acid, our kidneys don't produce base to neutralize. They retain H+ at the expense of K+, resulting in low potassium.
2. Drug Chelation- binding and preventing absorption of other drugs |
|
|
Term
|
Definition
|
|
Term
| What is the most common kind of ulcer? |
|
Definition
|
|
Term
| If the pain of an ulcer is worse after eating, what kind is it? If the pain is soothed by eating? |
|
Definition
Worse: Gastric Ulcer
Better: Duodenal Ulcer |
|
|
Term
| Continuous use of NSAIDS (like ibuprofen) can lead to what GI issue? Why? |
|
Definition
Gastric ulcer
They decrease prostaglandin production leading to ulceration |
|
|
Term
| What bacterium is often associated with the formation of gastric and duodenal ulcers? |
|
Definition
|
|
Term
| What type of drugs are used as anti-emetics? |
|
Definition
| 5-HT3 Antagonists, D2 Antagonists |
|
|
Term
| What does Ondansetron treat? How? |
|
Definition
| Ondansetron is an anti-emetic. It decreases activity in CTZ by decreasing serotonin (5-HT3). |
|
|
Term
| What is Scopolamine used for? What drug class does this belong to? |
|
Definition
| It is used as a patch for motion sickness. It belongs to the anticholinergic group. |
|
|
Term
| What is an example of a pro-emetic that works by stimulation of the CTZ? |
|
Definition
|
|
Term
| What is the MOA of bulking agents? Osmotic laxatives? |
|
Definition
Increased stool mass and volume
Draw water into colon to stimulate peristalsis |
|
|
Term
| What is Lubiprostone used for? What is its MOA? |
|
Definition
It is used as a laxative.
MOA: Lubricates colon, pumps chloride ions into the colon, water follows |
|
|
Term
| Why is diarrhea hard to treat? |
|
Definition
| The cause of diarrhea is very hard to determine as their is such a broad range of potential causes. (drugs, nutrition, IBS, allergy, etc.) |
|
|
Term
| What drugs are known for causing constipation and are therefore used to treat diarrhea? |
|
Definition
|
|
Term
| Why is Loperamide the opiate of choice for treating diarrhea? |
|
Definition
| It is peripherally restricted and cannot cross the blood brain barrier so it has a very low abuse risk. |
|
|
Term
|
Definition
|
|
Term
| What are the inputs and outputs in regulation of the CV system? |
|
Definition
Inputs are from afferent nerves and humoral agents, integrated in brainstem.
Outputs adjust heart, vascular and kidney functions (efferent). |
|
|
Term
| What is the number one cause of death in Americans? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Fatty streak within an artery |
|
|
Term
| What is atherosclerosis and how does it occur? |
|
Definition
It is a stiffening of the arteries.
Reduces the diameter of the lumen, can induce blood clot- due to plague, cholesterol, etc. |
|
|
Term
| Why are high levels of HDL cholesterol associated with lower risk of atherosclerosis? |
|
Definition
| HDL (good cholesterol) and their lipoproteins transport lipids back to the liver for catabolism. |
|
|
Term
| High concentrations of LDL is associated with? |
|
Definition
| Increasing severity of cardiovascular disease. |
|
|
Term
| How are apolipoproteins an example that all cholesterol is not bad? |
|
Definition
| They help transport HDL and are important for health because of some of their benefits (antioxidant, anti-inflammatory, etc.) |
|
|
Term
| What is Lovastatin? What does it do? |
|
Definition
| It is a statin- up regulates liver LDL uptake and reduces circulating LDL levels. (reducing cholesterol biosynthesis leads to increases in LDL receptors) |
|
|
Term
| What is the term for chronically elevated hypertension without a known cause? |
|
Definition
|
|
Term
| Sympathetic nerve activity increase is directly proportional to ____________. |
|
Definition
| Hypertension increase, of all kinds |
|
|
Term
| Diurnal BP pattern "dippers" are known to have a greater chance of what? Why is this problematic in drug administration? |
|
Definition
Stroke
Antihypertensives are typically taken in the AM, after rising. The BP surge when rising occurs at the same time as treatment and the medication taken the previous day may be less effective. |
|
|
Term
| T/F: A natural product is still considered such even if it can be made by total synthesis. |
|
Definition
|
|
Term
| What are some examples of natural products? |
|
Definition
| Plants, bacteria, fungi, animals,etc. |
|
|
Term
| T/F: Our drug pipeline still primarily consists of things from nature. |
|
Definition
|
|
Term
| What are some sources of variation in snake venom? |
|
Definition
| The type of snake, age, geographical location |
|
|
Term
| Why do snakes have voluntary control over how much venom they release? |
|
Definition
| They utilize careful titration because venom is very metabolically expensive to make. |
|
|
Term
| What is the only appropriate method of treating a snake bite? |
|
Definition
|
|
Term
| Where do venom components come from? |
|
Definition
| The venom comes from mutated body proteins within the salivary gland (ex: a heart gene which mutates and when turned on causes crardiotoxic effects) |
|
|
Term
| What is ACE? Where is it produced? What is its function? |
|
Definition
Angiotensin Converting Enzyme
In the lungs
To convert Angiotensin I to Angiotensin II |
|
|
Term
| Snake venoms are often used to make what kind of drug? What are some examples of this type of drug? |
|
Definition
ACE inhibitors
Captopril, Enalopril |
|
|
Term
| Where is angiotensin produced? Where is renin produced? What is their interaction? |
|
Definition
The liver
The kidney
Renin converts Angiotensin to Angiotensin I. |
|
|
Term
| What are some effects of Angiotensin II? |
|
Definition
| increase in sympathetic activity, retention of NaCl + water, excretion of K+, increase in blood pressure |
|
|
Term
What effect do ACE inhibitors (like in snake venom) have?
What could these be used to treat? |
|
Definition
They cause a very rapid drop in blood pressure.
They make great hypertension medications. |
|
|
Term
| What are the steps in column chromatography? |
|
Definition
| Fractionation, testing for activity, determining the structure of the activated peptide |
|
|
Term
| What group of people worked the structure of of ACE in order to determine specific sites of inhibition and synthesize it? |
|
Definition
|
|
Term
| What ACE inhibitor peptide was first found to be most effective and then synthesized? Why didn't it work? |
|
Definition
Teptrotide
It wasn't orally available |
|
|
Term
| What was the first clinical ACE inhibitor on the market? (first blockbuster ACE inhibitor) |
|
Definition
|
|
Term
| What are some medical uses of ACE inhibitors? |
|
Definition
| Hypertension treatment, cardiac failure, renal disease, systemic sclerosis, diabetic nephropathy |
|
|
Term
| Drugs ending in -pril belong to what group? |
|
Definition
|
|
Term
| T/F: There are no other sources for ACE inhibitors aside from snake venom. |
|
Definition
| False- there are other sources but they don't work as well |
|
|
Term
|
Definition
| The process of discovery + commercialization of new natural products. |
|
|
Term
| What are four kinds of natural product isolation that can be done at home? |
|
Definition
1. Distillation- water or oil
2. Extraction- using alcohol as solvent
3. Alcohol distillation
4. Pressing- mechanical manipulation |
|
|
Term
| What are the 7 antihypertensive agents? |
|
Definition
| Diuretics, ACE inhibitors, Ang II Receptor blockers, Ca2+ channel blockers, Beta Blockers, Alpha-adrenoceptor drugs, vasodilators |
|
|
Term
|
Definition
| They act on the kidneys to increase urine output, therefore lowering cardiac output as there is a lower stroke volume (less blood volume with less water). |
|
|
Term
| What are the three types of diuretics? Examples? |
|
Definition
1. Thiazides- Hydrochlorothiazide (HCTZ), block pump
2. Loop diuretics- Furosemide, sodium potassium pump block
3. K+ Sparing Diuretics- Amiloride, Spironolactone |
|
|
Term
| Losartan is an example of what kind of drug? How does this work? |
|
Definition
| It is an Angiotensin II blocker which works as an antihypertensive. By decreasing the effects of Angio II, we have a decrease in TPR and MAP. |
|
|
Term
| Nifedipine, Minoxidil, and Nitroglycerin are examples of what kind of antihypertensives? Which one not only works as an arterial dilator but also as a venous dilator (vasodilator)? |
|
Definition
They are Ca2+ channel blockers
Nitroglycerin also acts as a vasodilator. |
|
|
Term
| What drug acts to inhibit alpha 1 adrenoreceptors? What effect does it have? |
|
Definition
|
|
Term
| Clonidine is what kind of drug? How does it work? |
|
Definition
A2 agonist (antihypertensive)
It decreases sympathetic outflow |
|
|
Term
| What are some examples of Beta blockers? What are they used to treat? |
|
Definition
Propanolol, Metoprolol
They treat cardiac failure |
|
|
Term
| Which beta blocker is contraindicated in asthmatics? Which is cardioselective so it can be used in asthmatics? |
|
Definition
1. Propanolol
2. Metoprolol |
|
|
Term
| What are Milrinone and Digoxin used for? |
|
Definition
|
|
Term
| Why is chemotherapy not as effective as antibiotics? |
|
Definition
| Selective toxicity, our immune system, diagnostic complexity |
|
|
Term
| Explain how chemotherapeutic agents follow first order kinetics or log kill phenomenon. |
|
Definition
| A given dose of the drug kills a constant fraction of the cells with each administration. Usually needs to be given 4-5 times in order to kill all of the cells. |
|
|
Term
| What is intrathecal? Why do we use this for chemo administration sometimes? |
|
Definition
| To give a drug intrathecally is to admin directly to the spinal fluid. We give chemo this way so it can target cells which are hiding in the brain. |
|
|
Term
| What is pharmacologic sanctuary? |
|
Definition
| Some leukemic cells will escape and hide within the brain where conventional chemo cannot reach them. |
|
|
Term
| What are some common issues associated with chemotherapy (why does it fail)? |
|
Definition
| Pharmacologic sanctuary, resistance, toxicity to selves |
|
|
Term
| In what phase of the cell cycle will cells not respond to drugs because they are "resting"? |
|
Definition
|
|
Term
| How do antimetabolites interfere with cell proliferation to work as a chemotherapy agent? |
|
Definition
| The can compete with binding sites or can be incorporated into the newly synthesized DNA or RNA (which can be problematic). They can do so because they are structurally similar to endogenous chemicals. |
|
|
Term
| What phase of the cell cycle do antimetabolites work at? |
|
Definition
|
|
Term
| What are the three types of antimetabolites? |
|
Definition
| Folic acid analogues, pyrimidines, purines |
|
|
Term
| Methotrexate is what kind of drug? |
|
Definition
| It is an antimetabolite belonging to the folic acid analogues group. |
|
|
Term
| What role does folic acid play in cell replication? |
|
Definition
| It plays a pivotal role in purine and thymidylate synthesis which are both essential to the process. |
|
|
Term
| What is Methotrexates MOA? What is it effective against? What is one drawback? |
|
Definition
MOA: Inhibits dihydrofolate reeducate, the enzyme which converts folic acid to active form (tetrahydrofolic acid).
It is effective against Burkitt lymphoma, lymphocytic leukemia, breast cancer and choriocarcinoma.
It can become polymerized in the DNA. It is also given orally and very toxic against GI walls. |
|
|
Term
| What is typically given in conjunction with methotrexate to counteract some if its toxic effects? Why? |
|
Definition
Leucovorin (folinic acid)- a tetrahyro derivative of folic acid which is used to rescue normal, proliferating cells from the toxic effects.
Works by replenishing folic acid pools. |
|
|
Term
| What are examples of methotrexate resistance? |
|
Definition
1. Increased intercell dihydrofolate reductase levels.
2. Decreased affinity of dihydrofolate reductase for methotrexate.
3. Reduced methotrexate transport into cells |
|
|
Term
| Antimitotics, a chemotherapeutic agent, work by? What are the two types? |
|
Definition
Interfering with cell division (M PHASE!)
Vinca alkaloids and taxanes |
|
|
Term
| Paclitaxel is what kind of a drug? What is it effective against? |
|
Definition
Taxane, used as chemotherapy
Used against lung, ovarian, breast cancer |
|
|
Term
| What chemotherapeutic agent works by stabilizing/polymerizing the microtubules so that there may be no chromosomal desegregation? |
|
Definition
|
|
Term
| How do antibiotics interfere with cell proliferation to act as chemotherapeutic agents? |
|
Definition
| They can intercalate with DNA, inhibit Topo I + II, produce free radicals and are not typically cell cycle specific. |
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Term
| What are the two types of antibiotics used in chemo? Which is cell specific ? |
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Definition
Anthracyclines and Bleomycin
Bleomycin is cell specific |
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Term
| Which chemo drug is remarkable bright red and known for its cardiotoxicity? |
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Definition
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Term
| What is the MOA for Doxorubicin? What is it effective against? |
|
Definition
Inhibition of Topo II so DNA remains supercoiled and dies.
Used for breast cancer, lymphomas, acute lymphocytic leukemia |
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Term
| What are some examples of hormones being used as chemotherapeutic agents? |
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Definition
-Breast cancer that is estrogen dependent
-Can be used in tumor growth regression (estrogen being used to treat advanced prostate cancer) |
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Term
| What hormonal agent is the first line of treatment in estrogen receptor positive breast cancer? |
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Definition
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Term
| T/f: In order for Tamoxefin to be effective, the patients do not need to be tested for SERM (estrogen receptors) first. |
|
Definition
| False. They must have these receptors or it will not help. |
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Term
| Which drug used in targeted therapy directly targets the extracellular domain of HER2 growth receptors and is therefore used to fight breast cancer? |
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Definition
|
|
Term
| What is the most modern form of cancer therapy? |
|
Definition
| Gene therapy- modulate the immune system to attack cancer cells |
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Term
| Humphrey Osmond was a drug pioneer in what class of drugs? |
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Definition
| Psychomimetics. Created "psychedelics"with Alvis Huxley. |
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Term
| The earliest fossil remains depicting hallucinogens show what and where? |
|
Definition
| The San Pedro Cactus and found in Peru |
|
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Term
| When was the "golden age" of psychedelics research? |
|
Definition
| 50s-60s (CIA MKULTRA, etc.) |
|
|
Term
| What ended the golden era of psychedelics? |
|
Definition
| Richard Nixon signed controlled substances act- LSD became a Schedule 1 drug |
|
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Term
| What are the three classes of hallucinogens? |
|
Definition
Indole (Serotonin)- LSD, psilocybin, DMT
Catechole- Mescaline, MDMA
Dissociative anesthetics- PCP, ketamine |
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Term
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Definition
|
|
Term
| What are catechole structures similar to? |
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Definition
|
|
Term
| Where does mescaline bind? |
|
Definition
| The serotonin 5HT2 receptors- although it has a low affinity for them so it is less potent. |
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|
Term
| What are some effects of mescaline? |
|
Definition
| lasting about 10-12 hours, hallucinations, rise in temp, anxiety, pupil dilation |
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Term
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Definition
| MDMA acts on the serotonin transporters (SERT) to release large amounts of serotonin into the synapse. It is also an agonist at the 5HT-2 receptors in CNS. |
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Term
| What is one potentially fatal condition associated with MDMA overdose? |
|
Definition
| Serotonin syndrome- huge cascade of serotonin leading to tachycardia, muscle degredation, death. etc. |
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|
Term
| What are the sought after effects of MDMA? Negative effects? |
|
Definition
Euphoria, increased perception of closeness, hallucinations, increased physical activity
Negative: Jaw clenching, anxiety, insomnia, paranoia |
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|
Term
| What structure are indoles similar to? |
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Definition
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