Exam 2 (missing antibiotic stuff...for now) Flashcards
What is used to treat lymphomas?
Prednisone, Rituximab
What is the mechanism of Type 5 Phosphodiesterase inhibitors?
It inhibits PDE5 to allow for more cGMP (causes vasodilation). Muscarinic ACh > Nitric Oxide > cGMP.
What is good for seasickness?
Scopolamine and other muscarinic blockers
What is Tx for hypertension?
Clonidine (Alpha 2 agonist)
What are the side effects of beta blockers?
Increased airway resistance in the respiratory tract – CAUTION IN USE WITH AN ASTHMATIC PATIENT! Impair recovery from hypoglycemia; Increase VLDL and decrease HDL, Bradycardia, Mild sedation or depression, Cardiac decompensation, Caution in use in high cholesterol and diabetic patients!
What cancer drug is a powerful blistering agent?
Mechlorethamine
Which drugs Bind to microtubule protein and prevent polymerization?
Vinblastine and Vincristine (microtubule inhibitors)
Which drug has this MoA: Inhibits DNA polymerase. Also can be incorporated into cellular DNA
Cytarabine
Where are the nonsteroidal antigens drugs (anti-cancer)?
Flutamide, Nilutamide (can cause visual problems) Bicalutamide
What drug stops VEGF from stimulating new blood vessels?
Bevacizumab
Is tamoxifen cell-cycle specific or not?
Tamoxifen is NOT cell-cycle specific
Which adrenergic receptors lead to a blood pressure increase?
Alpha 1, Beta 1 (but there is a reflex decrease in HR)
What drug goes through P450 metabolism
Vinblastine and Vincristine and Docetaxel and Paclitaxel (microtubule inhibitors)
Curing cancer results in about ___% of patients. Overall 5-year survival rate for cancer patients is __%
10%. 65%
How do you test for Horner’s syndrome?
Use phenylephrine. If it doesn’t dilate then it’s probably not Horner’s. then test with ophthalmic cocaine: No dilation = postganglionic lesion. Dilation= preganglionic lesion.
What are the steps of ACh production and use?
1 Choline enters and 2 combines with Acetyl CoA through Choline acetyltransferase. 3 Ach put in vesicles. 4 AP causes Ca++ to enter the axon > 5 vesicle fuses with axon terminal. 6 ACh eventually gets broken down by AChE. 7 Choline gets recycled
Which adrenergic receptors lead to a blood pressure decrease?
Alpha 2, Beta 2
What is the first line therapy for breast cancer?
Tamoxifen
Which drugs are analogs of gonadotropin releasing hormone?
Leuprolide and Goserelin
Which antimetabolite is given orally?
6-mercaptopurine (and Methotrexate can be oral)
What drugs bind to tubulin subunits and make microtubules more stable (cells are stuck in metaphase)
Docetaxel, Paclitaxel
What are the adverse effects of Muscarinic blockers?
Mydriasis, Cycloplegia, Dry mouth, Tachycardia, Flushed skin, Agitation, Delirium, Elevated body temperature
What receptor stimulates the iris dilator muscle?
Alpha 1
What is Tx for asthma?
Albuterol, Metaproterenol, Terbutaline
What happens if the miotic pupil does not dilate with phenylephrine?
It’s probably not Horner’s syndrome, then
What can cause Crystalline retinopathy and other vision probs?
Tamoxifen
Which drugs are Cholinomimetic Alkaloids?
Pilocarpine, nicotine, muscarine
What happens when you activate Alpha 1 receptors?
Vasoconstriction in skin increases blood pressure, Iris dilator muscle dilates pupil, urine retention, slows GI tract (but contracts sphincters)
Are alkylating agents cell cycle specific or non-cell cycle specific?
Not cell-cycle specific
What are the properties of Choline esters?
ACh, Carbachol, Bethanechol are hydrophilic (poorly absorbed), Carbachol and Bethanechol are more resistant to AChE –longer duration of action
Which receptor targets the Vascular smooth muscle, pupillary dilator muscle, and heart?
Alpha-1
Which drug’s adverse effect? : Pulmonary toxicity Alopecia Hypertrophic skin changes and hyperpigmentation Fever and chills
Bleomycin
Which antibiotic cancer drug is cell cycle specific?
Bleomycin
AE: Hot flashes, nausea, vomiting, skin rash; Potential to cause endometrial cancer, Crystalline retinopathy and other vision problems
Tamoxifen
What kind of receptor is muscarinic?
g-protein.
Which drug has this MoA: Pyrimidine analog Forms a molecular complex that deprives the cell of thymidine (DNA synthesis stops)
5-fluorouracil
What are the effects of Beta blockers on the cardiovascular system?
Decrease in blood pressure in patients with hypertension (decrease in renin release), Slow atrioventricular conduction (Decrease heart rate and cardiac output). Can have an acute effect of increasing BP via the blocking of B2 mediated vasodilation
What are side effects unique to Direct-Acting Muscarinic Stimulants?
Nausea, Frontal headache (from accommodation stimulated), Urinary urgency, Salivation, Sweating, and flushing of the skin (vasodilation) . Both direct and indirect have Bronchial constriction, Vomiting, Diarrhea, convulsions
What adrenergic drugs are limited clinically?
Alpha 2 antagonists, but they are being used experimentally in diabetes and depression.
What’s good for advanced breast cancer?
Leuprolide and Goserelin
Which drugs can cause buildup of uric acid in the urine?
Vinblastine and Vincristine (microtubule inhibitors)
What are side effects unique to cholinesterase inhibitors?
Miosis, Salivation, Sweating, and Muscle weakness. Both direct and indirect have Bronchial constriction, Vomiting, Diarrhea, Convulsions,
What is still used to treat ED outside US? What mechanism?
Yohimbine! It’s alpha 2 antagonist that promotes NE release to increase sympathetic activation
Which drug has this MoA: Prevents folic acid conversion to THF leading to decreased DNA/ protein materials
Methotrexate
Which non-selective alpha agonist has greater affinity for alpha 1 over alpha 2?
Phenoxybenzamine
Which drugs contain a benzene ring with ethylamine side chain?
Sympathomimetic
AE: Severe nausea and vomiting Severe bone marrow depression Latent viral infections due to immunosuppression Patient will be very susceptible to infection. Must use caution.
Mechlorethamine
Nm nicotinic receptors are on ___
Skeletal Muscle
What can regenerate AChE?
Pralidoxime
What can cause chemical conjunctivitis at high doses?
Cytarabine (antimetabolite)
What are the clinical uses of alpha antagonists?
For tumors that secrete NE, hypertension, Urinary obstruction (enlarged prostate), ED
Which alkylating agent transforms into an active metabolite?
Dacarbazine
What drug induces cell-mediated cytotoxicity and must be infused slowly?
Rituximab
Why don’t we use nicotinic blockers?
They are too nonspecific and would cause major side-effects
What is the neurotransmitter and receptor of preganglionic parasympathetics? Long or short?
Long, Ach nicotinic
What are the clinical uses of Cholinomimetics in the Eye?
Glaucoma (pilocarpine and carbachol are older treatments)
What do muscarinic blockers do to the urinary tract and sweat glands?
Slows voiding. Reduces sweating
Which ANS receptors are nicotinic?
All pre-ganglionic cells (and somatic skeletal muscle motor end plates)
Which Antibiotic cancer drugs can be given subcutaneously, IM, or IV?
Bleomycin
What happens when you apply Direct-Acting Cholinoceptor Stimulants to the eye
Contraction of iris sphincter (miosis), ciliary muscle (accommodation), and opening of trabecular meshwork (lower IOP)
What do muscarinic blockers do to the lungs?
They cause Bronchodilation, a reduce secretions in lung
What is good treatment of Uveitis
Homatropine or Cyclopentolate
What Tx for certain lymphomas and leukemias?
Rituximab
What is the tissue target and actions for Alpha 1?
Vascular smooth muscle (contraction), pupillary dilator muscle (contraction – dilation), and heart (increase force of contraction)
How are Monoclonal antibodies administered.
NOT orally! IV
What is the short-acting Indirect Acting Cholinomimetic? How does it work?
Edrophonium. Forms reversible bond with the enzyme. Not actually a substrate for ACh-esterase
What receptor is only on the heart?
Beta 1
What happens when you apply Direct-Acting Cholinoceptor Stimulants to the heart and blood vessels?
Hyperpolarization of the SA and AV node (decreases AP and contractility), blood vessels release NO from endothelial cells to cause vasodilation
What receptor relaxes the smooth ciliary muscle?
Beta 2
What is the effect of activating muscarinic receptors of the GI tract?
Increased muscle tone and peristaltic activity
Name MOA: Forms a stable complex with DNA Intercalates into double helix between G-C base pairs Interferes with RNA polymerase and hinders DNA synthesis
Dactinomycin
Which receptors are rapid on/off and desensitize to constant activation?
Nicotinic receptors
<p>Which non-selective alpha antagonistcan potentially be used for ED treatment (injection)?</p>
<p>Phentolamine</p>
What are some problems associated with chemotherapy?
Resistance, multidrug resistance, toxicity
What Tx for prostate cancer?
Flutamide, Nilutamide (can cause visual problems) Bicalutamide [all nonsteroidal antigens]. Also Leuprolide and Goserelin
What does a selective receptor mean?
It can become non-selective at high concentration
Which drug is an estrogen antagonist?
Tamoxifen
What is good for myasthenia gravis?
Indirect acting Cholinomimetic (Edrophonium for diagnosis, pyridostigmine for treatment and neostigmine)
What do adrenoceptor antagonists do (heart, and other effects)
They block vasoconstriction, lowering blood pressure. This can result in orthostatic hypotension and reflex tachycardia. They also cause pupil constriction, cause nasal stuffiness, and increase urine flow
Which anti-metabolite is not used for maintenance therapy?
6-thioguanine
What is Tx for acute hypotension?
Alpha agonists (NE, Phenylephrine)
What are the intermediate-acting Indirect Acting Cholinomimetics?
Neostigmine, Physostigmine, Pyridostigmine
What is effect of an Indirect Acting Cholinomimetic on the NMJ?
prolong and intensify the actions of acetylcholine
What drugs are mutagenic and carcinogenic?
Alkylating agents
What happens when you apply Direct-Acting Cholinoceptor Stimulants to the NMJ?
Causes depolarization followed by depolarization blockade
What is the tissue target and actions for Alpha 2?
CNS and PNS nerve terminal (inhibits NT release). Also decreases aqueous production and increase uveoscleral outflow
What is effect of an Indirect Acting Cholinomimetic on the heart and vessels? What is the NET result?
Decrease heart rate and force of contraction (decrease in cardiac output and BP). Increase in vascular resistance (vasoconstriction causes increase in BP because of sympathetic ganglia stimulation). Net result is mild BP increase but high dose will cause BP to fall.
MOA: steroid that Triggers production of specific proteins that reduce cell growth and proliferation
Prednisone
What does sympathetic activity do to the blood vessels in skeletal muscle and in the skin?
Symp causes dilation in muscles but constriction in the skin
Which antimetabolite is used in low doses to treat inflammatory diseases: severe psoriasis, rheumatoid arthritis, crohn disease?
Methotrexate
What can cause vasoconstriction?
Alpha agonists (Epi, Phenylephrine, Tetrahydrozoline)
What is effect of an Indirect Acting Cholinomimetic on the CNS?
Low concentrations: alerting response. High concentrations: convulsions
Which antimetabolite is given topically for skin cancer and the prevention of scar formation?
5-fluorouracil
What is the tissue target and actions for Beta 2?
Respiratory, uterine, and vascular smooth muscle (Relaxes smooth muscle). Skeletal muscle (promotes K+ uptake)
What can treat cholinergic poisoning?
Atropine (muscarinic blocker)
What drugs bind guanine in DNA to form cross links?
Cisplatin, Carboplatin, Oxaliplatin
Which cancer drug basically activates the immune system?
Interferons
What are the long-acting organophosphates? Where are they distributed?
Echothiophate, Malathion, Parathion, Sarin. All are distributed to CNS except echothiophate
What does a specific receptor mean?
Specific means it will stay specific regardless of concentration
What drug class would be bad for an asthma patient?
Direct and indirect acting cholinoceptor stimulant, Timolol (beta blocker)
What is the neurotransmitter and receptor of preganglionic sympathetics? Long or short?
Short, ACh nicotinic
Which alkylating agent is given orally?
Lomustine
What is a treatment of testicular cancer?
Bleomycin with vinblastine or etoposie
What can be used for Alzheimer’s treatment?
Tacrine (not used as often due to side effects), Donepezil, Galantamine, Rivastigmine
What are the common adverse side effects of cancer treatment?
Severe vomiting, Bone marrow suppression, Alopecia, Myelosuppression (patient prone to infection)
AE of “other” cancer drugs: Mild nausea, myelosuppression
carboplatin and oxaliplatin
What kind of receptor are the Alpha and beta receptors?
G-protein coupled receptors
Which drug has this MoA: Inhibits the first step of purine-ring biosynthesis and blocks formation of AMP
6-thioguanine and 6-mercaptopurine
Where are alpha 2 receptors located?
On the presynaptic membrane. They are “autoreceptors”
Which antibiotic cancer drug can make red urine and dark red veins?
Doxorubicin
What are the ocular side effects of type 5 Phosphodiesterase inhibitors?
Mild impairment of color vision, Blurry vision, Increased risk of ischemia
Which Cholinomimetic alkaloid is toxic?
Muscarine
What happens when you activate Alpha 2 receptors?
Reduces NE release from preganglionic neuron, reducing sympathetic effects. Insulin release is inhibited
What happens if the cocaine drops cause dilation?
Horner’s syndrome is from preganglionic lesion
Which Cholinomimetic alkaloid can be absorbed across the skin?
Nicotine
Which cancer drug is hardly excreted?
Mechlorethamine
Why is a combination of drugs good for cancer treatment?
Provide maximal killing with tolerated toxicity, Effective against broad cell lines, May delay development of resistant cell lines. If use drugs with similar toxicities, dose of each must be reduced
What are the clinical uses of Cholinomimetics in the GI/urinary tract?
Postoperative atony, neurogenic bladder. Basically smooth muscle disorders where there is no obstruction. Pilocarpine and Cevimeline can increase salivary secretion in Sjogren’s syndrome.
Do Adrenergic receptors desensitize?
They are non-desensitizing
Which “steroid hormone and antagonists” are actually steroids? Which are not steroids?
STEROIDS:
What is a Pharmacologic Sanctuary?
A place where some tumor cells can “hide” in tissues where chemotherapeutic agents cannot enter. Radiation “finds” these tumors
Which antibiotic cancer drug goes through extensive liver metabolism?
Doxorubicin.
Which adrenergic receptors lead to an increase in heart contractility and heart rate?
Beta 1
Activation of what receptor causes bronchodilation?
Beta 2
What does sympathetic/parasympathetic activity do to the Kidney?
Sympathetic alters the secretion of renin. Parasympathetic does nothing
What can produce a fever in younger patients?
Muscarinic blockers
What do muscarinic blockers do to the GI tract?
Decrease salivation, production of stomach acid, smooth muscle tone and propulsive movements
Which adrenergic drug is effective in topical administration to the eye?
Timolol
What is effect of an Indirect Acting Cholinomimetic on the respiratory tract?
Basically the same as direct. Contraction of bronchial smooth muscle: Bronchoconstriction. Stimulation of bronchial glands: Increase mucous secretion. This would be bad for an asthma patient
What happens when you apply Direct-Acting Cholinoceptor Stimulants to the respiratory system?
Contraction of bronchial smooth muscle: Bronchoconstriction. Stimulation of bronchial glands: Increase mucous secretion. This would be bad for an asthma patient
AE: Delayed hematopoietic depression, development of aplastic marrow, renal toxicity and pulmonary fibrosis
Carmustine, Lomustine
What drug should not be given to people undergoing cataract surgery?
Tamsulosin because it can cause IFIS (Floppy iris syndrome)
Which cancer drugs are aromatase inhibitors?
Aminoglutethimide, Anastrozole and Letrozole, Exemestane
What is Log kill?
The concept that destroying cancer cells follows first-order kinetics (that a steady dose kills a constant FRACTION of cells)
Which drugs help increase survival after a heart attack?
Propranolol (Beta blocker), Timolol (beta blocker), Metoprolol (Beta 1 blocker)
What is the process of making NE?
Tyrosine > DOPA > Dopamine, which enters vesicles > NE via Dopamine β hydroxylase. NE is metabolized by MAO and diffused into surrounding tissue
What is Tx for chronic orthostatic hypotension?
Midodrine (Alpha 1 agonist)
What happens when you activate Beta 1 receptors?
Affects HEART: higher bp, heart rate, increase contractility. Affects Kidney too (more renin > increase blood volume because more water)
What do nonsteroidal antigens do?
Nonsteroidal antigens that compete with natural hormone for the androgen receptor and prevent translocation of the hormone into the nucleus
Which nonsteroidal antigens drug can cause visual problems?
Nilutamide can cause visual problems
Which receptor is an “autoreceptor”?
Alpha 2
Which drugs are the choline esters?
ACh, Carbachol, Bethanechol
Which drugs can cause anorexia?
5-fluorouracil and 6-mercaptopurine
What do muscarinic blockers do to the cardiovascular system?
Increase HR but no strong net effect
What is effect of an Indirect Acting Cholinomimetic on the Eye?
Basically the same as direct. Contraction of iris sphincter (miosis), ciliary muscle (accommodation), and opening of trabecular meshwork (lower IOP)
What do muscarinic blockers do to the eye?
They cause mydriasis (constrictor is inhibited), cause cycloplegia (ciliary muscle is inhibited), and reduce lacrimal secretion.
Which ANS receptors are muscarinic?
Only post-ganglionic receptors
What are common steroid effects?
Predispose patient to infection, Hyperglycemia, Cataract formation, increased IOP, Osteoporosis, Mood changes: hyper and happy
What is the neurotransmitter and receptor of postganglionic sympathetics? Long or short?
Long, NE alpha/beta
Which antimetabolite should be avoided in pregnancy ?
Methotrexate
What adrenergic receptor prevents urination?
Alpha 1
What is the distribution and elimination of muscarinic blockers?
Most are widely distributed through CNS. They are eliminated via the kidney.
Which cancer drugs tend to have fewer adverse effects?
Monoclonal antibodies because they can be directed at specific targets.
What is Tx for cardiac arrest?
Isoproterenol, Epinephrine
Which cancer drug treats melanoma?
Dacarbazine
Vomiting and diarrhea are uncommon for which anticancer drug?
Docetaxel and Paclitaxel
What is good for accurate refraction?
Homatropine or cyclopentolate
What is the neurotransmitter and receptor of postganglionic parasympathetics? Long or short?
Short, Ach muscarinic
What is the tissue target and actions for Beta 1?
Heart (increases force and rate of contraction)
AE: Severe vomiting, Nephrotoxicity, Ototoxicity
Cisplatin
Nn nicotinic receptors are on ___
Neurons
What are beta blockers used for clinically?
Hypertension, Ischemic heart disease by regulating heartbeat and decreasing O2 demand, Cardiac arrhythmias, Heart failure, Glaucoma, Hyperthyroidism, migraines, tremors and stage fright/anxiety
What can treat COPD and Asthma?
Ipratropium or Tiotropium
What happens when you activate Beta 2 receptors?
Bronchodilation, elevates blood glucose (via glycogen breakdown) and increases glucagon secretion from pancreas. Also decreases blood glucose via insulin. Relaxes smooth ciliary muscle to decrease accommodation.
Which cancer drug Sensitizes the patient to radiation (sun)?
Dactinomycin
What is good for dilated fundus exam?
Tropicamide or Cyclopentolate
What treats breast cancer?
First line treatment: Tamoxifen Aminoglutethimide, Anastrozole and Letrozole, Exemestane [all aromatase inhibitors]. For advanced breast cancer: Leuprolide and Goserelin [GnRH analogs]
Which antibiotic cancer drug can cause irreversible cardiotoxicity?
Doxorubicin
What can treat urinary urgency or bladder spasm?
Oxybutynin (Muscarinic blocker)
Which alkylating agent can penetrate the CNS?
Carmustine, Lomustine
What is the goal of chemotherapy?
Goal is to cause a lethal cytotoxic event or apoptosis in the cancer cell or arrest tumor’s progression
What happens if the cocaine drops do not cause dilation?
Horner’s syndrome is from postganglionic lesion
What was developed as a mustard gas during WWI
Mechlorethamine
AE: Severe reactions have been fatal: Must infuse slowly. Hypotension, bronchospasm, and angioedema; Chills and fever after first infusion; Cardiac arrhythmias; You don’t see nausea vomiting hair falling out
Rituximab
Cholinomimetic alkaloid are easily or hardly absorbed from administration sites?
Cholinomimetic alkaloid are EASILY absorbed from administration sites?
Which is more potent: Docetaxel, Paclitaxel?
Docetaxel
What receptor is on respiratory, uterine, and vascular smooth muscle and skeletal muscles?
Beta 2
