Unit 6 Drugs Random Order Flashcards
Saw Palmetto
Use: BPH
May be eff. but not as eff. as existing drugs (azosins”
Mech: Inh test synth (enz inh)+Inh test binding to receptor
SE:
- Minimal SE
- Drug interactions due to hormone effects
Aluminum hydroxide
Al(OH)3
Antacid
Speed-slow
Duration-long
Neutralizing-low
SE:
- Constipation
- Adsorbs drugs
- Loss of phosphate
- Al toxicity
Polyethylene glycol
GI Drug
Cathartic–Osmotic agent
DOC for colonoscopy
Castor oil
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Linaclotide
GI Drug
Cathartic–Secretion enhancer
Mech: Activate guanylate cyclase
Increase Cl secretion in stomach
Garlic
Uses: Decrease blood lipids
May slightly lower blood lipids
1 fresh clove/day
SE:
- Induce P450
- Bad breath
- Decrease clotting
- Decrease conc. of some reverse transcriptase inh.
Mg(OH)2
GI Drug
Cathartic–Osmotic agent
AKA Milk of Magnesia
Codeine
Tx: Diarrhea
Narcotic agent
Mech: act a specific receptor
Not generally used for obvious reasons
Digoxin
Emetic–central stimulant
Mech: Stimulates DA sites in CTZ
Sucralfate
GI drug-Enhance mucosal defense
Aluminum salt
Tx: Ulcers
Mech: Complex that becomes viscous and binds to damaged mucosa when exposed to acid
SE:
- Constipation
- Excess Al absorption
Contraindication: H+ depleters (PPI or antacids)
SucrALfate=ALuminum salt→Excess Al
Sucralfate=sucrose=sticky…so this sticks to damaged mucosa
Immunosuppressants for IBS
Methotrexate
Cyclosporine
Miglitol
Tx: Diabetes
Glucose abs. delayers
Mech: Inh. alpha glucosidase
Prevents breakdown of complex carbs in gut
SE:
- Unabsorbed carbs ferment in gut
- Cramps
- Diarrhea
- Flatulence
Mig--litol
_Midg_ets (Mack) are little b/c they don’t absorb any carbs
Dronabinol
Anti-emetic–THC derivative
Mech: Bind cannabinoid receptor
SE: Increased appetite
Calcitonin
Tx: Ca disorders
Mech: Binds to and inh. osteoclasts
Effects opposite of PTH
Secreted by thyroid gland
1st line of defense for Paget’s disease
SE:
- Increase risk of cancer
What are the short acting designer insulins?
Regular human insulin
Lispro
Aspart
Glulisine
2-5 hrs
Pramlintide
Tx: Diabetes
Amylin analogs
Mech: Activate amylin receptor→
Decrease gastric emptying
Decrease appetite
Route: SubQ before meals
SE:
- Severe hypoglycemia
- prAMLINtide=AMyLIN analog*
Scopolamine
Anti-emetic–anti-cholinergic
Mech: Block muscarinic receptor
Route: Patch
SE:
- Dry
- Drowsy
- Etc.
What are the gastric irritants used as cathartics?
Cascara
Senna
Castor oil
Bisacodyl
Psyllium
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Yohimbe
Use: ED
Mech: Alpha 2 blocker in CNS
SE:
- Hypertension
- MAOI
- CNS excitation
- Tachycardia
- Tremor
Ergocalciferol (D2)
Tx: Ca disorders
Mech: Vit D analog
Less potent than calcitriol
SE: Hypothyroidism
Tolbutamide
Tx: Diabetes
Oral hypoglycemic agents
First gen sulphonylureas
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Duration: 6-12 hrs
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
What are the stool softeners?
Dioctal sodium sulfosuccinate
Mineral oil
Alpha galactosidase
Tx: Diarrhea
Mech: Increase metab. of oligosacc.→digestible sugars
Oligosacc. produce gas
- Alpha GAlactoSidase inh. GAS production*
- *Be careful there are alpha-glucosidase inh in the diabetes section**
Misoprostole
GI drug-Enhance mucosal defense
Tx: Ulcers
Drop in PGs→Ulcer
Asprin (NSAIDs) and GCs can decrease PGs
Mech: Prostaglandin analog
SE:
- Uterine contractility (abortifacient)
- You eat miso soup when you have a stomach ache because it is prostagrandin anarog (say that w/ a strong asian accent)*
Which antihistamines are used as anti-emetics?
Diphenhydramine
Dimenhydramine
Meclizine
Cyclizine
-prazole
GI drug
Decrease acid formation
Mech: ATPase inhibitor
Known as proton pump inhibitor (PPI) but actually irreversibly inhibit ATPase required to drive H+ pump
Best available class of GI drugs
Prodrug-activated by acid
They are weak bases though→ stay in parietal cell
SE:
- Hypochlorhydria-lack of H+ production
- Decrease Ca absorption→osteoporosis
- Decrease Vit B12 absorption
Isophane
Tx: Diabetes
Designer insulin
Protamine insulin
Intermediate acting
Glargine
Tx: Diabetes
Designer insulin
Short acting (24+ hrs)
Determined to get large (that a long time)
Detemir +glargine=long acting insulins
-setron
Ondansetron
Granisetron
Dolasetron
Palonosetron
Anti-emetic (for IBS+chemo)
Mech: 5HT receptor blocker
Affect CTZ +rec. in gut
SE: Constipation
_SE_lective _T_e_R_minators _O_f _N_ausea
-SETRON
-setron blocks serotonin
Echinacea
Use:
- Upper resp. inf.
- Wound healing
- Antifungal
Can decrease sympt. of flu if used early
SE:
- Allergies
- Related to ragweed
Cinecalcet
Tx: Ca disorders + hyperparathyroidism
Mech: Calcium mimetic
Sensitizes parathyroid Ca receptors to Ca→Decrese PTH secretion
Like there is a lot of Ca around
SE
- Hypocalcemia
- Nausea
- Diarrhea
Fluoride
Tx: Ca disorders
Effects: Increase osteoblasts
Makes bone harder but more brittle
Not for osteoporosis
Cyclizine
Anti-emetic–Antihistamine
Mech: Block H1 receptor
SE: Anticholinergic effects
Diphenoxylate
Tx: Diarrhea
Narcotic agent
Mech: act a specific receptor
Acts primarily in gut
Opiate like effects in CNS though too
Given in comb w/ atropine to avoid abuse
Nabilone
Anti-emetic–THC derivative
Mech: Bind cannabinoid receptor
SE: Increased appetite
What are the osmotic cathartics?
MgSO4
Mg(OH)2
Polyethylene glycol
Compazine
Anti-emetic
Mech: DA blocker
*Related to anti-psychotic drugs *(phenothiazine)
SE: Extrapyramidal effects
Magnesium hydroxide
Milk of magnesia
Antacid
Speed-slow
Duration-medium
Neutralizing-high
SE:
- Laxative
- Some Mg toxicity
Cascara
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Ginseng
Uses: Increase energy
No clear effect
Scopolamine
Tx: Diarrhea
Anti-cholinergic agent
Mech: Blocks muscarinic receptor
SE: Many systemic
Aminobisphosphonates
other -dronates
Aminobisphosphonates are more potent
Tx: Ca disorder
Mech: Enzyme inhibitor (farnesyl pyrophosphate synthetase)
Inh. enzyme in mavalonic acid synthesis pathway→abnormal cytoskeletal structure in osteoclasts
Pyrophosphates have an affinity for Ca and are incorporated into bone
When ingested by osteoclasts→decrease activity and apoptosis
T1/2: Many years
Use: 1st line tx for osteoporosis and pagets
Used in tx of MM too
SE:
- GI upset, peptic ulcers
- Inflammation of eye
- IV infusions cause 1st dose effect (flu-like symptoms)
- Osteonecrosis of jaw
- Decrease blood flow to area
- Esp in pts w/ lost of dental disease/surgery
- Bone w/ bisphosphonates may be more susceptible to infections
Belly ache and peptic ulcers
Infections/Infarcts
Swollen eye
First dose eff (IV)→Flu-like symptoms
Osteonecrosis of jaw
Bisphosphonates
Tiludronate
Etidronate
Bisphosphonates are less potent
Tx: Ca disorder
Mech: Enzyme inhibitor
Cause formation of abnormal ATP→inh ATP requiring enzymes
Pyrophosphates have an affinity for Ca and are incorporated into bone
When ingested by osteoclasts→decrease activity and apoptosis
T1/2: Many years
Use: 1st line tx for osteoporosis and pagets
Used in tx of MM too
SE:
- GI upset, peptic ulcers
- Inflammation of eye
- IV infusions cause 1st dose effect (flu-like symptoms)
- Osteonecrosis of jaw
- Decrease blood flow to area
- Esp in pts w/ lost of dental disease/surgery
- Bone w/ bisphosphonates may be more susceptible to infections
Belly ache and peptic ulcers
Infections/Infarcts
Swollen eye
First dose eff (IV)→Flu-like symptoms
Osteonecrosis of jaw
Infliximab
Tx: IBS
Mech: Binds TNF alpha
Calcium carbonate
CaCO3
Antacid
Speed-rapid
Duration-medium
Neutralizing-high
SE:
- Constipating
- Hypercalcemia
Cranberry
Uses: UTI
May inh. recurrent UTI
Not helpful for current inf.
Mech: Proanthrocyanadin prevents bact from binding to UT cells
May also acidify urine
SE:
- Inh P450
Sodium Bicarbonate
NaHCO3
Antacid
Speed-rapid
Duration-short
Neutralizing-high
SE:
- CO2 production
- Belching
- Na may compromise low sodium diets
-
Systemic absorption
- Contains Na
- Important in those w/ kidney dysfunction
Bran
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Loperamide
Tx: Diarrhea
Narcotic agent
Narcotic DOC for diarrhea
Mech: act a specific receptor
Acts ONLY in gut–no CNS effects
Crofelemer
Tx: Diarrhea
Mech: Blocks Cl channel in gut
Also decreases secretion of Na and H2O
CrofeLemer blocks CL channels
- or *
- CROws block the CLouds*
- CROfelemer blocks CL channels*
Acarbose
Rosiglitazone
Pioglitazone
Tx: Diabetes
Glucose abs. delayers
Mech: Inh. alpha glucosidase
Prevents breakdown of complex carbs in gut
SE:
- Unabsorbed carbs ferment in gut
- Cramps
- Diarrhea
- Flatulence
- A-carb-ose*
- No-carb-abs.*
-gliptin
or
-glyptin
Sitagliptin
Saxagliptin
Linaglyptin
Alogliptin
Tx: Diabetes
Incretin enhancer
Mech: Inh DPP-4 Enzyme →prevent incretin metab
Orally
Often used in combo w/ other drugs
- Put a lip of dip in (oral). Dip comes in a tin*
- G-_LIP_-TIN are DPP inh. Taken orally.*
Valerian
Uses: Sedative
Mild sedative effect
Mech: Increase GABA
SE:
- Hepatotoxicity
- Dont use w/ anti-dep
Raloxifene
Tx: Ca disorders +estrogen dependent breast cancer
Mech: Activates estrogen receptors in bone
Blocks estrogen receptors in breasts
Estrogen analog
SERM-selective estrogen receptor modulator
Inh. osteoclast activity
SE
- Pulmonary embolisms
- Stroke
- Preg. cat X
- Raloxifene like Tamoxifene affect estrogen receptor*
- SE=SEX*
Stroke
Embolism (pulmonary)
X (preg cat.)
Metformin
Tx: Diabetes
Insulin enhancers
Mech: Act. protein kinase→
Increased glc abs. by muscle
Decreased glc production by liver
SE:
- Lactic acidosis (potentially fatal)
- Weight loss due to anorexia
- George Foreman was an American Professional (Kick)boxer *
- Metformin Activates Protein Kinase*
- He worked out so hard he had lactic acidosis and had to be anorexic to make his weight class*
Kola nut
Caffeine
Increased HR
Insomnia
Bismuth subsalicylate
GI drug-Enhance mucosal defense
Anti-diarrheal agent–absorbing agent
Mech: Increase mucous production in stomach
Inh. growth of H. pylori
Unpleasant taste+odor
SE:
- Long term use→Darkening of feces, tongue, and teeth
What are the bulk adding agents?
Bran
Methylcellulose
Polycarbophil
Psyllium
Meclizine
Anti-emetic–Antihistamine
Mech: Block H1 receptor
SE: Anticholinergic effects
Gli–ide
or
Gly–ide
Glipizide
Glyburide
**Glimepiride **(most potent)
Tx: Diabetes
Oral hypoglycemic agents
Second gen sulphonylureas
More rapid onset and longer duration
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE: Less than 1st gen
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
-gliflozin
Canagliflozin
Dapagliflozin
Empagliflozin
Tx: Diabetes
Inh. of glc resorption by kidney
**Mech: **Inh. SGLT2 (Na-glc cotransporter)
in PCT–allows kidney to eliminate blood glc
SE:
- Hypotension
- Hypokalemia
- Due to increased urine output
- Gential fungal inf
- Urine loaded w/ glc
Senna
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Soy
Uses:
- Hyperlipidemia
- Osteoporosis
- Menopause
Decreases LDL
Decreases Menopausal symptoms
Mech: Metab. to estrogen like compound
SE: Allergic rxns
Diphenhydramine
or
Dimenhydramine
Anti-emetic–Antihistamine
Mech: Block H1 receptor
SE: Anticholinergic effects
(Apo)morphine
Emetic–central stimulant
Mech: Stimulates DA sites in CTZ
Dioctal sodium sulfosuccinate
GI Drug
Cathartic–Stool softener
Detergent
Mech: Emulsifies contents of colon
Mineral oil
GI Drug
Cathartic–Stool softener
Mech: Acts like a lubricant
Why mineral oil should NOT be used:
- Prevents fat soluble vitamin absorption
- Aspiration pnemonia →may damage lungs
- May contain carcinogens
Regular human insulin
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Afrezza is the inhaled form
Tolazamide
Tx: Diabetes
Oral hypoglycemic agents
First gen sulphonylureas
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Duration: 12-60 hrs
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
Lispro
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
St Johns Wort
Uses:
- Mild depression
- anxiety
As eff as standard anti-dep.
Mech: Inh. reuptake of NE, 5HT, DA
SE:
- Phototoxicity
- Other allergic rxns
- In breast milk→lethargic baby
- Induces P450
- Wafarin
- BC
- Anti-depressant interactions
Bisacodyl
GI Drug
Cathartic–Gastric Irritants
Mech: Stimulate gastric nn
Increase motility
Decrease electrolyte secretion into gut
SE:
- Nephritis
- Liver damage
Glulisine
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Denosumab
Tx: Ca disorders
Mech: Blocks a receptor (RANKL)
RANKL required for osteoclast production, activity, and survival
Given every 6 mnths
SE:
- Hypocalcemia
- Osteonecrosis of jaw
- Skin inf.
Deno- SHO
Skin inf.
Hypocalcemia
Osteonecrosis
Atropine
Tx: Diarrhea
Anti-cholinergic agent
Mech: Blocks muscarinic receptor
SE: Many systemic
-glutide
**Liraglutide **(Inj 1x/day)
Albiglutide (Inj. 1x/week)
Tx: Diabetes
Incretin enhancer
Mech: Bind to and activate receptors on B cell
Incretin analog
SE:
- Thyroid tumor
- I want my glutes to be as hard as concrete*
- -glutide to be as hard as incretin*
-glitazone
Rosiglitazone
Pioglitazone
Tx: Diabetes
Insulin enhancers
Mech: Act. PPAR→
Increased insulin receptor response
Increased # insulin receptors
Increased glc uptake by cells
SE:
- Wt gain
- Edema
- Fractures of arms and legs
- Macular edema
- Cardio problems
- MI
Exenatide
Tx: Diabetes
Incretin enhancer
Mech: Bind to and activate receptors on B cell
Analog of GLP-1 (incretin)
Not broken down by DPP-4
Injection 2x/day
SE:
- Pancreatitis
Chlorpropamide
Tx: Diabetes
Oral hypoglycemic agents
First gen sulphonylureas
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Duration: 60+ hrs
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
-glinide
Repaglinide
Nateglinide
Tx: Diabetes
Oral hypoglycemic agents
Sulphonylurea-like agents
Rapid onset, short duration
Mech: K channel blockers
Bind diff site on K channel
Block K channels on B cells →Increase Ca→Insulin secretion
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
Erythromycin
Tx: Gastroparesis
prokinetic agents–agents that increase stomach emptying rate
Mech: Acts directly on motilin receptor
Route: Oral but IV possible if oral is not
SE:
- ototoxicity
- pseudomemb. colitis
- cardiac arrythmia
- Especially if metabolism is inh by P450
- Remember erythro is a macrolide*
- Motiliy*
- Arrythmias*
- Cholesteric toxicity (liver tox)/Colitis*
- Restricts P450*
- Ototoxicity*
Glucocorticoids
Effects: Inh. osteoblasts
So bone loss
Antibiotic combo for H pylori infection
GI drug-Enhance mucosal defense
Metronidazole
+/-
Amoxicillin
+/-
Clarithromycin
+/-
Tetracycline
Alvimopan
Tx: Gastroparesis
prokinetic agents–agents that increase stomach emptying rate
Mech: Blocks opiate receptor in gut but not anywhere else
Blocks constipation due to post op opioid use
Simethicone
Tx: Diarrhea
Mech: Changes gas surface tension of gas pocket in gut
MgSO4
GI Drug
Cathartic–Osmotic agent
Difenoxin
Tx: Diarrhea
Narcotic agent
Active metabolite of diphenoxylate
Mech: act a specific receptor
Acts primarily in gut
Opiate like effects in CNS though too
Given in comb w/ atropine to avoid abuse
Ginko
Uses:
- Dementia
- Intermittent claudication–pain in leg
About as eff. as tacrine for tx of alzheimer’s
But tacrine isn’t really effective at all
SE:
- Inh platelet activating factor
- Decrease clotting
- Interacts w/ warfarin
Methylcellulose
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Flax oil seeds
Uses:
- Constipation
- Diarrhea
- IBS
- Diabetes
- Arthritis
- Atherosclerosis
- Menopause
May slightly lower total cholesterol
May decrease hot flashes
Mech: Soluble fiber and phyto estrogens
SE:
- Increase GI act.
- Allergic rxns
Polycarbophil
GI Drug
Cathartic–Bulk adding agent
Mech: Like eating fiber
Ipecac
Emetic–reflex stimulant
Mech: Act. receptors in GI mucosa
Instant severe vomiting
SE: Cardiotoxic
Teriparitide
Tx: Ca disorders
Mech: PTH analog
Increase osteoblast activity
Daily subQ injections for short periods
High doses→osteoclast stimulation so only given in short bursts
SE-increase incidence of osteosarcoma
Which GCs used for IBS
Prednisone
Budesonide
Lubiprostone
GI Drug
Cathartic–Secretion enhancer
Mech: Acts on PGE receptor
PGE1 derivative
Also acts on Cl channel in intestine
Detemir
Tx: Diabetes
Designer insulin
Long acting (24+ hrs)
Determined to get large (that a long time)
Detemir +glargine=long acting insulins
Heparin
Effects: Act. osteoclasts
So bone loss
-tidine
GI drug
Decrease acid secretion
Mech: H2 receptor blockers
SE:
- Confusion in elderly
- Bradycardia
Cimetidine:
- Inh. P450
- Prevent synth of test.
- Anti-androgenic
- Cause gynecomastia
Ma huang (ephedra)
Use:
- Weight loss
- Nasal congestion
- Asthma
- Increase athletic performance
Strong CNS stimulant
SE:
- Stroke
- Hypertension
- MI
Metoclopramide
Tx: Gastroparesis
prokinetic agent–agents that increase stomach emptying rate
Also used for hiccups
Mech: DA and possible 5HT antagonist
Route: Oral or IV
Increase motility w/o secretion (of H or gastrin)
SE:
- Sedation
- Depression
- Parkinson like symptoms
Metoclopramide increases motility
- All that motility→shakes (parkinson like symptoms)*
- All those shakes →sedation *
- All that sedation→depression *
Paracalcitrol
Tx: Ca disorders
Mech: Vit D analog
Less potent than calcitriol
SE: Hypothyroidism
-sala-
Sulfasalazine
Mesalamine
Olsalazine
Balsalazide
Tx: IBS–Salicylates
Mech: Decrease PG synth
Online it says mech is unclear–may not be the same as aspirin
Not systemically absorbed-like a topical drug for the stomach
SE:
- Diarrhea
- Take 3-5 weeks to work
Aspart
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
What are the long acting designer insulins?
Detemir
Glargine
