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121 Cards in this Set
- Front
- Back
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Histamine is stored in _________ of _______ cells
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Granulocytes
Mast |
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Histamine is highly _______ small molecule
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polar
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Histidine is de________ to produce histamine
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Decarboxylated
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Histamine exists in the body as 70% ______ 30% ______ based on which nitrogen of the imidazole is protonated
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70% tele (distal N)
30% pro |
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pka of ethylamino portion of histamine is ____ while the imidazole nitrogen portion is __
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ethylamino 9.4
imidazole N 5.8 |
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At physiologic pH histamine exists as a __________ species, whereas at stomach pH it is _________
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monocationic
dicationic |
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Dicationic histamine has affinity for ____ receptors
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H-2
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H-2 antagonists have these properties to compete against dicationic histamine
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heterocyclic species with increased lipophilicity but additional polarity
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Histamine is metabolized by
s-adenosyl methionine (_________) or by _________ and __________ |
methyltransferase
oxidative deamination + aldehyde dehydrogenase |
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Less sedating H-1 antagonists are characterized by increased ________
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polarity
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gastric ulcers form at these areas while duodenal ulcers localize at the duodenum
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fundus, corpus, pylorus, antrum
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peptic cells produce this proenzyme
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pepsinogen
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vagus nerve stimulation of ___ receptors indirectly increases ________ cells release of histamine
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M1
endrocrine |
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_________ cells produce HCl in the stomach
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parietal
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HCl provides the ideal pH 2 to convert ________ to _______ allowing for the breakdown of protein in the stomach
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pepsinogen - pepsin
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_________ cells line the wall of the stomach with mucin and also releases ________
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pyloric
bicarbonate |
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Therapeutic areas to treat peptic ulcers
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Buffering Agents
H2 antagonists Anticholinergics Proton Pump Inhibitors Cycloprotective agents |
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Antacids work to convert strong acids to _________ via reaction with the salt of a _______
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weak acid
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HCl + NaHCO3 ----->
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NaCL + (H2CO3) ---> H2O + CO2
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Common cations for salts of weak acids
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Na
Mg Ca Al |
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Systemic considerations of sodium salts
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Very soluble - absorption
systemic alkalosis urine alkalinization |
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Though sodium bicarbonate is often used as a buffering agent (antacid) it is detrimental to peptic ulcer disease because
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Conversion into CO2 causes bloating
Rebound acidity due to induction of HCl secretion |
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Mg salts can cause ________
Al salts can cause ________ Mylanta combines both salts to offset these effects |
Mg - diarrhea
Al - constipation |
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A decrease in the basicity of the urea-like group on H-2 antagonists will ________ potency
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increase
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Cycloprotective agents work by
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PGE1 derivatives increase mucin secretion
Mimick mucin with non-reducing sucrose |
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Phenbenzamine
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1st Gen H-1 Antagonist
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Diphenhydramine (Benadryl)
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1st Gen H-1 Antagonist
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Pyrilamine (Nisaval)
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1st Gen H-1 Antagonist
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Chlorpheniramine (Chlortrimeton®)
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1st Gen H-1 Antagonist
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Brompheniramine (Dimetane®)
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1st Gen H-1 Antagonist
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Triprolidine (Actifed®)
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1st Gen H-1 Antagonist
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Cyclizine (Marezine®)
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1st Gen H-1 Antagonist
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Chlorcyclizine
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1st Gen H-1 Antagonist
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Meclizine (Antivert®)
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1st Gen H-1 Antagonist
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Hydroxyzine (Atarax®)
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1st Gen H-1 Antagonist
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cetirizine (Zyrtec®)
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2nd Gen H-1 antagonist
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Clemizole (Allercur®)
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1st Gen H-1 antagonist
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Phenthiazine
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1st Gen H-1 antagonist
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Promethazine (Phergan®)
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1st Gen H-1 antagonist
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Trimeprazine (Temaril®)
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1st Gen H-1 antagonist
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Pimethixene
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1st Gen H-1 antagonist
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Methixene
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1st Gen H-1 antagonist
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Cyproheptadine (Periactin®)
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1st Gen H-1 antagonist
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Azatadine (Optimine®)
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1st Gen H-1 antagonist
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Terfenadine (Seldane®)
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2nd Gen H-1 antagonist
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Fexofenadine (Allegra)
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2nd Gen H-1 Antagonist
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Acrivastin (Semprex®)
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2nd Gen H-1 Antagonist
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Astemizole (Hismanal®)
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2nd Gen H-1 Antagonist
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Cetirizine (Zyrtec®)
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2nd Gen H-1 Antagonist
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Loratadine (Claritin®)
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2nd Gen H-1 Antagonist
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Cromolyn
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Miscellaneous Antiinflammitory
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PPi's are effective in treating this type of stomach cancer
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Alison-Zolinger
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Omeprazole (Prilosec®)
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Proton Pump Inhibitor
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Lansoprazole (Prevacid®)
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Proton Pump Inhibitor
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Esomeprazole (Nexium®)
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Proton Pump Inhibitor
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Pantoprazole (Protonix®)
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Proton Pump Inhibitor
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Cimetidine (Tagamet®)
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H2 Blocker
least potent - 400mg CYP inhibitor kills sperm |
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Ranitidine (Zantac®)
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H2 Blocker
intermediate potent - 150mg |
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famotidine (Pepcid®)
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H2 Blocker
most potent - 20mg |
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nizatidine (Axid®)
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H2 Blocker
intermediate potent - 150mg |
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H2 blockers shouldn't be taken with _________ for peptic ulcers
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Antacids
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misoprostol (Cytotec)
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Cycloprotective Prostaglandin
short acting contraindicated in pregnancy |
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sucralfate (carafate)
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Cycloprotective Agent
non-reducing sucrose w/ aluminum sulfate |
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Most common ions involved in nerve signal transmission
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K
Ca Na |
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K is usually found _______ nerve membrane while Ca and Na are normal ________
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inside
outside |
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The outer layer of the sodium channel is rich in negatively charged ________ residues
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Glutamate
Aspartate |
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The middle of the sodium channel is highly lipophilic due to ________ residues
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Tryptophan
Phenylalanine |
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Local anesthetics are commonly used for:
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Dental procedure
Rectal hemorrhoids Topical burns / itch Sore throat Eye irritation Inflitration anesthesia |
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Why are injections of local anesthetics often co administered with epinephrine?
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Epinephrine increases duration of action and decreases cardiotoxic effects by constricting movement away from the area of injection
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Cocaine
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Local anesthetic: ester
not used - abuse potential |
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Procaine (Novacaine®)
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Local anesthetic: ester
dental - short acting 15min 2hrs w/ epinephrine |
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Why is procaine contraindicated with sulfa antibiotics?
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Procaine is an ester injection anesthetic, metabolism by esterases will increase PABA. Sulfa antibiotics work by decreasing PABA to prevent DNA synthesis of purines.
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Tetracaine (Pontocaine®)
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Local anesthetic: ester
1-3hr |
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Proparacaine (Alcaine®, Ophthetic®)
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Local anesthetic: ester
eye solution |
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Cyclomethycaine (Surfacaine®)
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Local anesthetic: ester
rectal cream 2-3hr |
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Dibucaine (Nupercaine®)
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Local anesthetic: benzamide
burns,hemorrhoids t1/2 - 5hr |
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Lidocaine (Xylocaine®)
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Local anesthetic: anilide
t1/2 - 1-1.5hr |
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Anilides are _____ stables toward HYDROLYSIS by AMIDASE than amides
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less
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Mepivacaine (Carbocaine®, Polocaine®)
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Local anesthetic: anilide
t1/2 = 2hr |
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Bupivacaine (Marcaine®)
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Local anesthetic: anilide
t1/2 = 3-4hr |
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Etidocaine
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Local anesthetic: anilide
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Prilocaine
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Local anesthetic: anilide
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Pramoxine (Tronothane®)
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Local anesthetic: ether
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Dyclonine (Dyclone®)
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Local anesthetic: ketone
oral solution |
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N__ of Guanine residues is a very _______ site for alkylating agents to bind.
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N7
neutrophilic |
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When an alkylating agent (electrophile) binds to N7 on a guanine residue it acts as an ______ _____ converting guanine into its ______ form.
This form of guanine resembles adenosine. |
electron sync
lactim |
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Alkylating agents were designed on the basis of autopsies from soldiers exposed to nitrogen gas.
A reduction in cancer cells was seen in autopsies. In order to decrease toxicity for possible treatment, Sulfur was replaced with ______ because it is more _________ decreasing its reactivity. |
nitrogen
electronegative (less electrons available for arizidine) |
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The addition of electron withdrawing groups to alkylating agents would ________ toxicity
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decrease
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In order to make alkylating agents more selective, _________ can be added.
Melphalan contains ________ |
amino acids
phenylalanine |
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Cyclophosphamide acts as a prodrug because ________ withdraws electrons to a degree that will inhibit activity until it is metabolized in the ________
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phosphate
liver |
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Cyclophosphamide
Cancer cells use _________ to break down _____________ into acrolein and active metabolite. |
B-elimination
4-hydroxycyclophosphamide |
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Cyclophosphamide is less toxic to normal cells (excluding bone marrow) because they can ________
4-hydroxycyclophosphamide into __________ for excretion. |
oxidize
carboxycyclophosphamide |
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Acrolein is toxic to bladder cells as they contain _______ groups. Mesna is used more often with _________ because it requires a higher IV dose due to its low potency, thus producing more acrolein.
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sulfhydryl groups
Ifosphamide |
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Thiotepa was designed to increase selectivity to cancer cells as they tend to be more ________ charged.
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negatively
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Polyglutamate synthetase will work to ________ cellular entry of folic acid
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maintain / increase
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This 1st generation H1 antagonist has high anticholinergic effects, and is formulated as a _____ salt
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Diphenhydramine (Benadryl)
HCl salt |
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Chlorpheniramine and Bromopheniramine are ____ sedating than other 1st gen H1 antagonists, and have ___ t1/2 due to blockade of _______
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less
longer para-hydroxylation |
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Triprolidine (Actifed) contains a double bond which increases rgidity. This would ______ conformational change and ____ in binding.
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prevent
aid |
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Most (not all) H1 antagonists ending in "zine" indicate a _______ nucleus which tends to target the ____
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piperazine
CNS |
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Meclizine ( Antivert) contains a piperazine and is often used for _______
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motion sickness
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This 1st gen H1 antagonist contain piperazine has high sedative effects and can be used as a tranquilizer.
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Hydroxyzine (Atarax)
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Aminobenzimadazole with a pyrolidine side chain. Placing two rings out of planes with eachother increased its binding to H1
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Clemizole (Allercur)
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These 1st gen H1 antagonists are thiazine-tricyclics and can cause sedation, hallucinations.
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Phenthiazine
Promethazine Trimeprazine |
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This 2nd gen H1 antagonist exists as a racemic mixture
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Cetirizine (Zyrtec)
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Cromolyn requires multiple daily dosing and must be given ______ to allergic response.
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Prior
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Loratidine (Claritin) is metabolized into ________ which is metabolized into active metabolite with ______ properties.
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desloratidine (clarinex)
zwitterionic |
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Order of decreasing electron withdrawal strength:
A. -SO2NH B. -CN C. -NO2 |
A > C > B
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Lidocaine (Xylocaine) is hydrolyzed by ______ into _____ + glycine
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amidase
xylene |
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Thymidine synthesis (de novo) requires __________ as co-factor which will convert back to ______ in the process.
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methylene THF
DHF |
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Methotrexate inhibits _______ which will decrease the conversion of _____ into dTMP by ______ ______. Build up of dUMP will convert back to _____ and integrate into DNA. Repair mechanisms will destroy DNA.
This destruction is termed _______ |
DHFR
dUMP thymidylate synthase dUTP "Thymine less death" |
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Leucovorin works to increase _______ synthesis in normal cells decreasing ____ toxicity.
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thymidine
MTX |
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5-FU and 5-UDR directly inhibit ________.
Capecitabine is a prodrug of 5-FU that resembles ______ converted by _________, _____, and ______ |
thymidylate synthase
5' deoxy - cytidine esterase CDA (cytidine deaminase) TP (thymidine phosphorylase) |
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Capecitabine:
Thymidine phosphorylase hydrolyzes _________ bond between 5' deoxyribose and _______ |
glycosidic
5-FU |
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Ara-C
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Analog of cytidine with an aribose sugar.
conformation resembles deoxyribose - phosphorylation leads to chain termination |
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Ara-C can be acted on by _____ to create an inactive metabolite _____ that cannot incorporate into DNA.
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CDA (cytidine deaminase)
Ara-U |
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Gemcitabine
5-Azacytidine 5-FU FUDR Capecitabine Ara-C |
Anti-metabolite: Pyrimidine Antagonists
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Triazine analog of cytidine metabolized to the triphosphate form to integrate into RNA. Also blocks DNA _________.
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5-Azacytidine (Vidaza)
methylation |
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_________ contains a geminal carbon and can be activated via ______, deactivated via ______, and also acts as a _______ _______ inhibitor.
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triphosphorylation
CDA ribonucleotide reductase |
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True or False
6-MP + 6-TG substrates for xanthine oxidase |
False
only 6-MP |
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6-MP
6-TG Azathioprine Fludarabine Cladribine Pentostatin |
Anti-metabolite: Purine Antagonists
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Fludarabine Phosphate and Cladribine are resistant to ______ and inhibit DNA replication.
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CDA
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