-
Cimetidine
H2 agonist on parietal cells (tagamet)
renal impair equals low dose
Most side effects of any H2
anti androgenic
-
Famotidine
H2 antagonist on parietal cell (pepcid)
renal impair equals low dose
-
Magnesium compounds
Longer action than NaHCO3
up Mg in blood
Cathartics and up intestinal motility
-
Nizatidine
H2 antagonist on parietal cell
Renal impair= now dose
-
Ranitidine
H2 antagonis on parietal cells
Inhibits acid by gastrin, muscarinic agonists and basal and meal induced
- down volume of juice
- down pepsin, down IF
Renal impair equals low dose
-
Sodium Bicarb
Baking soda
short acting
transient metabolic alkalosis
Na+ load= fluid retention
exacerbated GERD, belching
Not for: GERD, peptic ulcers, HTN
-
Sucralfate
Complex Al-sucrose sulfate
Coats ulcer
Acid/pepsin barrier
No-antacid effect
Stimulates prostaglandin E
activated by acid environmenbt
lower availability of tetracycline, phenytoin, digoxin, cimetidine
-
rabeprazole
least metabolized CYP2D1A
rapid onsed
PPI
before meal
-
omeprazole
PPI
OTC
before meal
-
Pantoprazole
PPI
before meal
-
Dexlansoprazole
PPI
before meal
-
Esomeprazole
PPI
before meal
-
Lansoprazole
PPI
before meal
-
Anthraquinones
Stimulant/irritant laxative
aloe, senna, cascara
-
Alosetron
5HT3 antagonist
severe IBS
Nausea, bloating, pain
Bad: constipating
-
Bismuth subsalicylate
pepto bismol
may prevent colonization w/ e. coli
prostaglandin= diarrhea
inhibit cox=antimotility
bad: tinnitus, constipate
-
difenoxin
active compound of opiate diphenoxylate
-
Diphenoxylate
and atropine= lomotil
opiate for diarrhea
inhibits pre-synaptic cholinergic neurons in submucosal and myenteric plex.
Few systemic side efx
-
Dicyclomine
Anticholinergic for IBS muscarinic
Anti-spasmodic
-
Hyoscyamine
Anti-cholinergic for IBS
anti-spasmodic for pain and discomfort
inhibit muscarinic receptors nin myenteric plexus and smooth muscle
-
Loperamide
opioid (imodium)
doesn't cross BBB
inhibit pre-synaptic cholinergic neurons in submucosal and myenteric plexus
for diarrhea
-
Agar
Hydrophilic colloid
Chronic constipation
-
Lactulose
Osmotic agent
Flatulence
-
Docusate
Stool softener
Allow H2) and lipids to penetrate
-
Bran
hydrophilic colloid
chronic constipate
-
Mag sulfate
osmotic agents
CHF=change in intravasc. volume
-
Sorbitol
Osmotic agent
Flatulence
-
Psyllium
Hydrophilic colloids
Chronic constip
-
polyethylene glycol
Colonic cleansing before endoscopy
balanced= no electrolyte shifts
-
methylnaltrexone
opiate antagonist for opiate constipation
does not cross BBB
-
Methylcellulose
hydrophilic colloids
1st line chronic constipation
-
Lubiprostone
Chloride channel activator
For: chronic constipation
Up liquid into lumen, shortens transit
-
Metoclopramide
D2 receptor antagonist
Inhibie smooth muscle stim
Up peristaltic amplitude
Up lower esophageal sphincter pressure
enhance gastric empty
low transit tiimes
For: anti emetic
-
Tegasrod
5-HT4 agonist
Stimulates 2nd order neurons of myenteric plexus=peristalsis
-
Lorazepam
Benzo
Before chemo for anxiety and anticipaqtory vomit
-
Diazepam
Benzo
Prior to chemo for anticipatory vomit
Reduce vomit from anxiety
-
Aprepitant
Neurokinin antagonist
NK1 antaqgonist= first ever cancer chemo and PONV
Used w/ serotonin agents
blocks action of substance P
-
Dronabinol
Cannabinoid antiemetic
1st pass hepatic meetab
appetite stim
For: chemo w/ others
Bad: euphoria, dysphoria, sedate, hallucinate, potentiates psychoactive
-
Scopolamine
Anti-muscarinic anti emetic
1st line for motion sickness
transdermal patch
-
Meclizine
antihistamine anti emetic
Bad: sedation, drowsy, dry mouth, urine reatin, cycloplegia
-
Promethazine
Antimistamine anti emetic
sedation, dry mouth, confuse, urine retain, cycloplegia
-
Droperidol
D2 antagonist
antipsychotic and sedative
antiemetic via central domamine
Bad: proarrythmic, extrapyramidal, hypotension
-
Metoclopramide
D2 receptor antagonist
Central dopamine block
Bad: Extrapyramidal, restless, dystonia
-
Prochlorperazine
inhibits dopaminergic, muscarinic, and histaminergic
Anti emetic via central dopamine blockade
Bad: Sedative=histamine
-
Dolasetron
5HT3 antagonist
vagal stim emesis
Acute chemo, surg, rads
-
Granisetron
5HT3 antagonist
vagal stim emesis
acute surg, rads, chemo
-
Ondansetron
5ht3
Intestin vagal afferents, and central receptors in vomit center and CTZ
Only emesis from vagal stim.
Acute chemo, rads, surgery
Bad: HA, dizzy, constipate
-
Thiabendazole
- For cutaneous larva migrans
- S. stercoralis
Also nematode trichinosis, T. spiralis (does not destroy larva in muscle)
Inhibits glucos uptake, acute reductase
adults, eggs, larva
Bad Olfactory, disturb, crystalluria, leukopenia, hallucinate, Stevens-Johnson, hepatic
-
Pyrantel Pamoate
For: nematodes
depolarizes myoneural junct. Spastic paralysis
Worms alone whjen passed
poorly absorbed= less toxic
Bad: no preggo, less y/o, or w/ piperazine
-
Praziquantel
For: all cestode and trematode
Up permeability to Ca2+
Impairs attachment
40mg/kg initially, lethal only for adults
Treat whole house
Bad: fever sedation, HA, abd. discomfort
-
Oxaminaquine
Alt. drug for trematode S. mansoni
Converted to unstable ester yielding reactive electrophiles
-
Niclosamide
For: cestodes- tapeworms
Inhibits glucose uptake
Causes detachment and pooping out
oral but not absorbed so up conc in intestines
-
Metrifonate
Alt for treamatode S. haemotobium
Organophosphate inhibitor of cholinesterase
Insecticide
Treat urinary schistosomas in africe
Inhibits plasma cholinesterase or host
Bad: vertigo, lassitude, nausea, colic
-
Mebendazole
For: most GI nematodes- pinworms
given to all household members
Inhibits glucose uptake adult t regg inhibits microtubule poly by B-tubulin
Oral but poor absorbed
Abd. discomfort and diarrhea
Not: preggo
-
Ivermectin
For: nematodes, O. volvulus, and S. stercoralis
Tonic paralysis of peripheral musculature
Potentiates GABA
Not in meningitis
Bad: itching, swollen glands, postural hypo, CNS
-
Diethylcarbamezapine
For: microfilaria, W. bancrofti, B. malavi, L. Loa in blood
Alt for nematod, O. volvulus
No effect for adult worm or microfilaria in lymph node
Hyper polarizes helm. muscle
Alters surface membanes
May cause system rxn from massive kill, start with small dose.
Encephalopathy w/ L. Loa
-
Bithionol
For CDC only
For: trematode F. hepatica
Also- chinese liver flukes
oral
Bad: vomit, diarrhea, uticaria, photosensitivity
-
Albendazole
New, broad spectrum anti helinthic.
Aot for hookworkm pinworm, porkworms, and threadworms
Drug of choice: hydatid dz, cysticercosis
Inhibits glucose uptake in helm. kills adults and eggs
Take- empty stom- for intraluminal w/ fatty- tissue
Not: preggo
-
Terbinafine
Synthetic allylamine
Inhibits fungal squalene eposidase.
Accumulates squalene epoxide (toxic)
Bad: GI upset and headache
daily for 12 wks= 90% rare
on chymycosis
better than griseo
-
Griseofulvin
Inhibits fungal mitosis by producing multinucleated cells.
Interacts w/ polyenergized microtubules
Bad: now w/ prophyria, induces liver enzymes, anti-inflammation
Teratogen and carcinogen
For: skin infections, microsporum, trichophyton, epidermophyton
-
Caspofungin
Echinocandin
Disrupts fungal cell wall synthby inhibiting B-(1,3)-D- glucan synth .
very expensive
Refractory invasive aspergillosis
-
Clotrimazole
Toxic and old
Ulsed topically
0.5%- skin
3-10%- vaginal
-
Posaconazole
Newest and very expensive
Broad spectrum
For: aspergillosis
Available as oral suspension
-
Itraconazole
Newer than kero
less toxic and broader spectrum
-
Fluconazole
triazole
Inhibits sterol 14-alpha-dmethylase
Greater GI absorb, cross BBB
Bad: no endocrine effects, N/V, renal, hepatic
Relapse cryptomening..
Prophylax in AIDS for candidiasis
-
Ketaconazole
imidazole
inhibits sterol 14 alpha demethylase
- absorbed well from GI
- H2 blockers down absorption
Bad: N/V, menstrual irreg, gynecomastia renal insuf. and heptotox
For: non-meningeal syst. blusto, histo, cocciolis
-
Flucytosine
inside fungal cell deaminated to 5FU anoalog of deoxyuridylic acid
5FU blocks thymidylate synthase
well abosrbed GI and corss BBB
Bad: bone marrow suppress, up LFT
-
Nystatin
Polyene
Same as Amp B.
K+/mg++ pore
only topical
For: candidiasis
-
Amphotericin B
Polyene
forms ion channel K+ Mg++
Binds ergosterol
No GI abosrption
Monitor renal-creatinine
Bad: neurotox, hypersiensitivity
For: life threatining mycotics
-
Artesunate
Water soluble arteminins
- P. falciparum
- iron from heme reduces peroxide bond
-
Artemether
Lipid soluble artemisinis
WHO drug
Worldwide for P. falciparum
iron form heme reduces peroxide bondin artemisinis
= high valent iron-oxo spears
-
Chloroquine
Aralen phosphate
Suppressive trends and acute uncomplicated malaria
effective against erythrocytic forms so ameliorates symptoms.
Fast acting- afebrile ulcer 1-2d
Blocks synth DNA and RNA
Oral/IV Protoporphyrin IX
Slowing divided doses
MDR durg resist
Not in: Psoriasis and porphyria
-
Quinine
Cinchona alkaloid
Clinical cure against severe chloroquine resistant P. falciparum
Best for cerebral malaria
Not by itself
Weak base- accumulates in food vacuoles
Bad: HTN, cinchonium - sweat, tinnitus, blurred vis, blood dyscrasias, hypoglycermia
Not: myasthenia gravis, tinnitus and optic something.
-
Metronidazole
Geniutal trichomoniasis
Intes6tinal and hepat6ic amoebiasis
Asymptomatic amebiasis
Drug of choice - giardiasis
+ electron sink in protozoa, nitro group reduced
Oral, IV = Up levels CSF
Bad: metallic taste, neurotoxin, red brown urine, urethral burning, phlebitis
Not: preggo, alcohol, CNS dz, dyscrasias, preggo
-
Dehydroemetine
Alt. drug for amebic hepatitis and amebic abscess
Followed by chloroquine and iodoquinol
Cardiovascular effect, UI tox, weakness, neuropathy
Not: w. preexisting cardio, muscular, neuro
-
Quinacrine
Used for: giardiasis 90% cure rate
Binds DNA through an intercalation. prevents synth of nucleic acid blocking DNAand RNA poly
Oral
Bad: yellow stain of skin and sclera. blue and black pigment in nail beds.
-
Mefloquine
Mulitdrug resistant P. flaciparum, as suppressive and clinical.
affects membranes
only give for short time to avoid reistance
Bad: 50%= dizzy, ataxia, and HA Neuropsych
-
Atovaquone and Proquanil
For: uncomplicated cases of multiresistant as a suppressive and clinical agent
Interferes w/ 2 diff path in pyrimidine biosynth
Inhibits mitochondrial, ETC, and dihydrofolate reductase
Take w/ food or milk- not with tetracycline
-
Quinidine
Antiarrythmic drug
Dextrostereoisomer of quinine
Anti-malarial
-
Diloxanide furoate
Drug of choice for asymptomatic amebiasis - only from CDC.
Well tolerated, some GI, pruritis
-
Sodium Stibogluconate
Pentavalent antimonial
Drug of choice for all 3 forms leishmaniasis
inhibits phosphofructokinase IV, IM, oral infiltrate
Bad: myalgia, ECG, pruritus, rash, myocardial damage
-
Pyrimethamine
Chloroquine-resistant infections
Not in acute setting by itself
Inhibits dihydrofolate reductase blocks purine and pyrimidines.
Synergistic w/ sulfonamides
Bad: flase acid problems, S/S if given w/ sulfaloxine
-
Doxycycline
a tetracycline for suppressive therapy against multi drug reistant
P. falciparum
Pts nable to take mefloquine
acute malaria w/ quinine
Active against blood stages but not liver stages
-
Emetine
Alt. drug amebic hepatitis and abscess.
Then use chloroquine and iodoquinol
Severe amebic dysentery-cannot cure
Replaced METRANIDOZOLE
Inhibits proetin synth by blocking chain elongation- prevents translocation
SQ or IM
Bad: CV effects- arrhythmias, EKG changes, GI tox, muscle weak, peripheral neuropath
-
Nifurtimox
Acute and chronic CHAGAS dz
Superoxide radical
oral
Adverse w/ EtOH
Bad: HA, insomnia, convulsions, myalgia
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