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161 Cards in this Set
- Front
- Back
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What does aspirin inhibit?
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- Cyclooxygenase
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What does methotrexate inhibit?
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- Dihydrofolate reductase
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What does tranylcypromine inhibit?
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- Monoamine oxidase
- It is an anti-depressant |
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What does nitroglycerin activate?
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- Guanylate cyclase
- Treats angina |
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What does heparin activate?
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- Anti-thrombin III
- It is an anti-coagulant |
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What does cocaine inhibit?
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- NE uptake by neurons
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What does chlorothiazide inhibit?
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- Sodium transport in the kidneys
- It is a diuretic |
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What does fluoxetine inhibit?
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- Serotonin uptake by neurons
- It is an anti-depressant |
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What does omeprazole inhibit?
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- Hydrogen ion transport by parietal cells of the stomach
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What ion channel does Nifedipine block?
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- Calcium channel blocker
- Used as an anti-hypertensive med. |
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Minoxidil is an agent that acts on an ion channel, so which ion does it uptake?
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- Increases K+ uptake by smooth muscle
- Used as an anti-hypertensive |
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What ion channel does Procaine inhibit?
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- Inhibits sodium channels
- Local anesthetic |
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Which receptor does Propanalol block? Is it an intracellular or extracellular receptor?
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- Beta blocker
- Extracellular receptor |
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Which receptor does Cimetidine block? Is it an intracellular or extracellular receptor?
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- Histamine (H2) receptor blocker
- Extracellular receptor |
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Which receptor does Prazosin block? Is it an intracellular or extracellular receptor?
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- Alpha-1 receptor blocker
- Extracellular receptor |
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What receptor does Morphine activate? Is it an intracellular or extracellular receptor?
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- Opiate receptor activator
- Extracellular receptor |
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What receptor does Insulin activate? Is it an intracellular or extracellular receptor?
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- Activates insulin receptors
- Extracellular receptor |
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What is the function of Glucocorticoids? Does it act on intracellular or extracellular receptors?
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- Activates receptors
- Intracellular receptor |
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What are 3 receptor characteristics?
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- Sensitive
- Selective - Specific cell response |
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What do we call a pharmacological agent that activates a receptor?
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- Agonist
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What do we call a pharmacological agent that inhibits a receptor?
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- Antagonist or receptor blocker
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What do we call a pharmacological agent that binds to a receptor but doesn't fully activate the receptor?
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- Partial agonists
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What do we call a pharmacological agent that can block the constitutive or inherent low level activity of a receptor?
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- Inverse agonists
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What is tachyphylaxis?
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- Very rapid desensitization to the effects of a drug
- Often due to depletion of tissue factor |
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The maximum effect of a drug is termed what?
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- Efficacy
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The effect of a drug relative to dose is termed what?
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- Potency
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The dose of a drug that causes a maximum effect in 50% of the subjects tested is termed what?
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- ED50 of a drug
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The dose of a drug that causes a toxic effect in 50% of subjects is termed what?
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- TD50 of a drug
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What is the ratio used to calculate the therapeutic index?
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- TD50 / ED50 or LD50 / ED50
- LD50 = lethal dose |
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T / F: The smaller the therapeutic index, the safer the drug?
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- False, the larger the therapeutic index the safer the drug
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What route of administration is safe, easy, can be self-administered but is irregular and unpredictable in absorption, has a slow onset, requires consciousness, and could cause GI upset or irritability?
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- Oral route of administration
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What route of administration is very rapid and accurate in dosage but can be painful, cause infection, and its effects are irreversible?
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- Parenteral route of administration
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What are the 3 parenteral routes of administration? Which is the slowest, which is the fastest
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- Subcutaneous = slowest
- Intramuscular - IV = fastest |
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T / F: The IV drug bioavailability = 100%
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- True
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What are the 3 mechanisms for drug entry into cells?
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- Passive diffusion
- Facilitated diffusion - Active transport / pinocytosis |
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T / F: Ionized drugs pass through membranes much more rapidly
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- False, non-ionized drugs pass through membrane more rapidly
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What is the Henderson Hasselbach Equation?
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- HA <--> H+ + A- = for weak acid
- BH+ <--> H+ + B = for weak base |
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T / F: Drugs bound to proteins within plasma,such as albumin, are readily metabolized and reach the active or target site
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- False, drugs bound to proteins don't reach the active or target site and are not readily metabolized
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What is the most significant site of drug metabolism?
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- Liver
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What is the name of the complex of enzymes in the liver that help with metabolism of drugs?
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- CYP 450
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What are the 3 Phase I reactions that the CYP450 complex does?
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- Oxidation
- Hydroxylation - Dealkylation |
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T / F: Deamination, Hydrolysis, Peptidases, Phosphatases, Alcohol dehydrogenases are all examples of Phase I, Non-CYP 450 reactions.
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- True
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Name the 5 Phase II reactions.
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- Glucouronidation
- Acetylation - Methylation - Glycine conjugation - Sulfation |
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What is the main function of diuretics?
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- Causes the net excretion of Na+ and H20 from the body, causing increased urine flow.
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In a normal kidney, what 3 things are reabsorbed into the blood from the PCT?
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- Na+ (65%)
- HCO3- - Ca2+ |
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In a normal kidney, what 3 things are reabsorbed into the blood from the ascending loop of henle?
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- Na+ (25%)
- K+ - Cl- |
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In a normal kidney, what 3 things are reabsorbed into the blood from the DCT?
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- Na+ (15%)
- Cl- - Ca2+ |
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Where is the Na+ / K+ exchanger located? What is it normally affected by that induces Na+ and K+ channels as well as Na+ / K+ ATPases?
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- Located between the DCT and Collecting Duct
- Affected by aldosterone |
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Where is the ADH / vasopressin receptor located in a normal kidney? What is its function?
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- In the Collecting Duct
- ADH: opens water channels and reabsorbs water back into the blood |
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T / F: The higher the concentration of ions in the kidney filtrate, more H20 will be eliminated?
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- True
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What are 2 examples of thiazide diuretics?
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- Chlorothiazide (Diuril)
- Hydrochlorothiazide (Hydrodiuril) |
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What portion of the kidney do thiazide diuretics act on?
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- Distal Convoluted Tubule (DCT)
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What is the mechanism of action for thiazide diuretics?
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- Inhibits NaCl transport in the DCT
- Resulting in an excess of Na+ and H20 in the kidney tubule that will be excreted in the urine, leading to hyperosmolar urine |
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What are 2 results from using thiazide diuretics?
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- Cause vasodilation: useful for hypertension therapy
- Decreases excretion of Ca2+: preserves bone mineral density |
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What are 4 side effects that could result from using thiazide diuretics?
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- Hypokalemia (K+ loss): excess Na+ reaches the exchanger resulting in more K+ lost from blood
- Decrease in uric acid excretion=gout - Inhibit insulin secretion - problem in Type II diabetics, will become hyperglycemic - Contains sulfur ions that may cause an allergic reaction |
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Drugs such as: Furosemide, Ethacrynic acid, Bumetanide, Torsemide act on what part of the kidney?
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- Ascending Limb of Loop of Henle
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What is the mechanism of action for Ascending Loop Diuretics? What are some uses of these diuretics (3)?
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- Inhibit NaCl + K+ reabsorption, even more so than thiazides
- Has a rapid onset of action - Uses: 1. Patients refractory to thiazide 2. Patients with decreased renal function 3. Patients with life threatening edema: cerebral / pulmonary edema |
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What are some side effects (5) from using Ascending Loop Diuretics?
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- Dehydration
- Severe hypokalemia - Increase calcium excretion in urine - Decrease uric acid secretion- gout - Auditory nerve damage |
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Name 2 aldosterone antagonists. What is their mechanism of action
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- Spironolactone (Aldactone)
- Eplerenone (Inspra) - Blocks aldosterone receptor therefore prevents Na+ reabsorption and K+ secretion |
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What are 2 side effects of using aldosterone antagonists?
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- Hyperkalemia
- Gynecomastia (males) / menstrual irregularities (females) |
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What part of the kidney do Triamterene and Amiloride act on? What is their mechanism of action? What is 1 side effect?
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- Na+ / K+ exchanger
- Prevent Na+ from entering principal cells, thus preventing the Na+ / K+ exchanger from reabsorbing Na and excreting K+ - Does not depend on aldosterone - Hyperkalemia = side effect |
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T / F: Potassium sparing diuretics (Spironolactone + Eplerenone) and Inhibitors of Na+transport in DCT and CD (Triamterene + Amiloride) are not very efficacious by themselves and are often used in combination with thiazides.
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- True
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Acetazolamide is an example of what type of diuretic? Where does it act on in the kidney?
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- Carbonic anhydrase inhibitor
- Acts on Proximal Convoluted Tubule (PCT) |
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Name 4 uses of carbonic anhydrase inhibitors?
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- Glaucoma: prevents formation of aq. humor
- Mountain sickness: decreases formation of CSF that is causing cerebral edema - Epilepsy - Alkalinize urine |
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Give 1 example of an osmotic diuretic. How is it given? What is its mechanism of action?
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- Mannitol
- Given through IV - It is a non-absorbable sugar that gets into the tubule, increasing water in the tubule and increasing osmolarity |
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What are some uses (2) for osmotic diuretics?
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- Maintain urine flow after traumatic injury
- Decrease CSF fluid volume and intracranial pressure |
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What is an example of a methylxanthine?
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- Caffeine
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What effect does ethanol have on the kidneys?
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- Inhibits the release of ADH and thus prevents the body from re-absorbing water
- This is why alcohol dehydrates you |
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Between the sympathetic NS and parasympathetic NS, which one has long pre-ganglionic neurons and short post-ganglionic neurons?
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- Parasympathetic NS
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Between the sympathetic NS and parasympathetic NS, which one has short pre-ganglionic neurons and long post-ganglionic neurons?
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- Sympathetic NS
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T / F: All pre-ganglionic neurons use ACh as a neurotransmitter.
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- True
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T / F: All post-ganglionic sympathetics use ACh as a neurotransmitter.
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- False, use NE and E
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T / F: All somatic neurons use ACh as a neurotransmitter and they do not have post-ganglionic fibers.
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- True
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T / F: All post-ganglionic parasympathetics use NE and E.
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- False, they use ACh
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The following physiological symptoms: pupil enlargement (mydriasis), decreased gastric motility, increased sphincter tone, increased HR, vasodilation of blood vessels to skeletal muscles, relaxed bronchial smooth muscle, relaxed bladder, ejaculation, describe what between the Sympathetic and Parasympathetic NS?
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- Sympathetic NS
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The following physiological symptoms: pupil constriction (miosis), increased gastric motility, decreased sphincter tone, decreased HR, relaxed blood vessels, constricted bronchial smooth muscle, contracted bladder and erection describe what between the sympathetic and parasympathetic NS?
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- Parasympathetic NS
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What type of neurotransmitter do cholindergic neurons secrete? How is action by the neurotransmitter terminated? Give examples of cholinergic neurons.
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- ACh
- Action is terminated by Acetylcholinesterase - All pre-ganglionic neurons = cholinergic |
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What type of neurotransmitter do adrenergic neurons secrete? How is action by the neurotransmitter terminated (3 ways)? Give examples of adrenergic neurons.
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- NE
- Action is terminated by Monoamine oxidase (MAO), catecholmethyl transferase (CoMT), NE taken back up at pre-synaptic site - Post-ganglionic sympathetic neurons |
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What are the 2 cholino-receptor subtypes?
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- Muscarinic receptors
- Nicotinic receptors |
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What type of cholino-receptor is linked to second messengers, usually via G proteins? They are also located at the end of organs in the parasympathetic NS?
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- Muscarinic receptors
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What type of cholino-receptor is linked to ion channels (ionotropic)? They are also located at the end organs in the somatic NS and at the ganglia in sympathetic and parasympathetic nervous systems.
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- Nicotinic receptors
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Name the 3 Adreno-Receptor Subtypes.
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- Alpha ( 1 and 2)
- Beta (1 and 2) - Dopamine (1 and 2) |
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T / F: All Adreno-Receptor Subtypes are ionotropic.
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- False, they are all linked to 2nd messengers.
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Name the 3 muscarinic agonists that are direct acting. What nervous system would they activate-sympathetic or parasympathetic?
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- Muscarine
- Pilocarpine - Bethanechole - Activate parasympathetic NS |
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Name the 2 direct acting nicotinic agonists.
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- Nicotine
- Succinylcholine |
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Name the direct acting partial nicotinic agonist.
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- Varenicline (Chantix) - binds to receptor but gets less stimulation
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Name 2 direct acting agonists that act on both nicotinic and muscarinic receptors.
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- Acetylcholine
- Carbachol |
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What is the action of all indirect-acting cholinergic agonists? How do we classify them?
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- All inhibit acetylcholinesterase - prevent the breakdown of ACh
- Classify them based on duration of action |
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What 3 indirect acting cholinergic agonists have a moderate duration and form covalent bonds with the enzyme?
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- Physostigmine (Eserine)
- Neostigmine (Prostigmin) - Demecarium |
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What indirect acting cholinergic agonist has a short duration and does not form covalent bonds, it is reversible?
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- Edrophonium (Enlon)
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What indirect acting cholinergic agonist has a long duration and it phosphorylates the enzyme, almost irreversibly modifying the enzyme?
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- Echothiophate (Phospholine)
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What are indirect acting cholinergic agonists used to treat (3 things)?
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- Glaucoma: increase aq. outflow
- Myasthenia gravis: flood muscle with ACh - Sjrogens syndrome |
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Name the 2 indirect acting cholinergic agonists that help treat Alzheimer's patients.
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- Donepezil (Aricept)
- Tacrine (Cognex) |
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Name 2 other uses (not tx or alzheimers) of indirect acting cholinergic agonists.
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- Insecticides: Malathion
- Nerve Gases: Sarim - They both irreversibly phosphorylate |
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What indirect acting cholinergic agonist can reverse phosphorylation?
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- Pralidoxine
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Name 8 toxicities of cholinergic agonists ("DUMBBELS").
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- Diarrhea
- Urination - Miosis - Bradycardia - Bronchoconstriction - Excitation of CNS - Lacrimation: increase - Salivation: increase |
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Name 2 cholinoreceptor blocking agents.
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- Anti-muscarinic agents
- Anti-nicotinic agents |
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What anti-muscarinic agent is derived from the plant Atropa belladona, has a long duration of action (7+ days), and causes mydriasis / pupil enlargement.
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- Atropine
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What anti-muscarinic agent lasts 3-7 days?
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- Scopolamine
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What 3 anti-muscarinic agents last for several hours?
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- Homatropine
- Cyclopentolate - Tropicamide = most common |
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What anti-muscarinic agent is used to treat asthma because it causes bronchi to open up?
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- Ipatropium
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What are some side effects of anti-muscarinic agents?
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- Increase tears
- Dry mouth - Bronchodilation - Urinary tension - Mydriasis - Decreased sweating - Increased HR - CNS effects - nausea, psychosis |
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Name the antinicotinic ganglionic blockers (2). What is their method of action.
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- Trimethaphan
- Mecamylamine - Complete autonomic blockade |
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What type of skeletal muscle nicotinic receptor blocker is succinylcholine? What is its function?
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- Depolarizing agent
- Inhibits muscle contraction, therefore it is a paralytic agent used in surgery |
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What type of skeletal muscle nicotinic receptor blocker are pancuronium, atracurium, and rocuronium? What do they cause?
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- Non-depolarizing agents
- Cause rapid paralysis |
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What does sugammadex do?
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- It is an agent that binds to Rocuronium and is used in case of an overdose
- It can also bring someone out of paralysis post-surgery |
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The botulinum toxin is an inhibitor of what release?
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- Inhibitor of ACh release
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Name the sympathetic adrenoreceptor subtypes and list where each is found.
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- Alpha 1 = found in vascular smooth muscle and heart to increase contractility and eye to increase aq. outflow
- Alpha 2 = presynaptic nerve terminals in the CNS- decrease release of NE - Beta 1 = Heart - Beta 2 = Lungs |
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What is the adrenergic agonist that acts on all adrenergic receptors (Alpha and Beta)?
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- Epinephrine
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What is the adrenergic agonist that activates alpha-1 receptors?
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- Phenylephrine (Neo-Synephrine)
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What are the adrenergic agonists that activate the alpha-2 receptors?
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- Clonidine
- Alpha-methyl norepinephrine |
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What are the adrenergic agonists that activate the beta-1 receptors?
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- NE
- Dobutamine |
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What are the adrenergic agonists that activate beta-2 receptors?
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- Metaproterenol
- Terbutaline - Fenoterol - Albuterol |
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Name the 5 indirect acting amines, which induce the release of NE from nerve terminals.
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- Amphetamine
- Tyramine - Phenylpropanolamine - Pseudoephedrine - Hydroxyamphetamine |
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What are the 2 adrenergic antagonists that are alpha-1 receptor blockers?
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- Prazosin
- Phenoxybenzamine |
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What is the adrenergic antagonist that is an alpha-1 and alpha-2 receptor blocker?
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- Phentolamine
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What is the adrenergic antagonist that is an alpha-2 receptor blocker?
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- Tolazoline
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What are the adrenergic antagonists that are beta-1 specific receptor blockers? The olol's.
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- Metoprolol
- Acebutolol - Alprenolol - Atenolol - Esmolol |
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What are the adrenergic antagonists that are beta-1 and beta-2 non-specific?
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- Propanolol
- Timolol - Levobunolol - Carteolol - Metipranolol |
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What is the ratio that's classified as normal BP?
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- 120/80
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What is the ratio that's classified as stage I hypertension?
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- 140 / 90
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A blood pressure of 160 / 100 is classified as what stage of hypertension?
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- Stage II hypertension
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A blood pressure of 180 / 110 is classified as what stage of hypertension?
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- Stage III Hypertension
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What is the ratio that's classified as life-threatening blood pressure?
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- 220 / 120
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What is the etiology of secondary hypertension?
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- Secondary hypertension has a clearly defined cause such as renal disease, pheochromocytoma, or drugs
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What is the etiology of primary (essential) hypertension?
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- Primary hypertension has an unknown etiology, it may be multiple etiologies
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How long does BP have to be elevated for to be classified as malignant hypertension?
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- 6 months or longer
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A decrease in blood pressure causes the sympathetic system to become activated. What 2 adreno-receptors become activated?
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- Beta-1 adreno-receptor on the heart
- Alpha-1 adreno-receptor on smooth muscle |
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What does activation of a Beta-1 adrenoreceptor do to increase blood pressure?
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- Increases cardiac output
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What does an alpha-1 adreno-receptor do to increase blood pressure?
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- Increases peripheral resistance
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A decrease in blood pressure decreases renal blood flow which activates what?
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- Renin
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Activation of renin ultimately leads to activation of what that causes vasoconstriction and in increase in blood pressrue?
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- Angiotensin II
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What does angiotenin II stimulate that leads to increased renal sodium reabsorption, increased blood volume, and increased blood pressure?
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- Aldosterone
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What are the 2 central alpha-2 agonists that act primarily on the CNS?
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- Alpha-methyl DOPA
- Clonidine |
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What central alpha-2 agonist may lead to a hypertensive crisis if suddenly withdrawn?
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- Clonidine
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What central alpha-2 agonist can be used in opiate withdrawal cases, neuropathic pain, insomnia, and turrets?
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- Clonidine
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What are the 3 anti-hypertensive agents that have central and peripheral effects?
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- Propanolol
- Reserpine - Alpha-methyl tyrosine |
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What are 2 anti-hypertensive drugs that block transmission at the ganglion?
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- Mecamylamine (Inversine)
- Trimethaphan camsylate |
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What anti-hypertensive drug effects the post-ganglionic neuron and acts by depleting catecholamines in peripheral and central neurons?
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- Reserpine
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What are the 3 Alpha-1 blockers that prevent NE from acting on alpha-1 receptors on vasculature?
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- Prazosin
- Terazosin - Doxazosin |
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What are the 3 Alpha-1 blockers that are used only for the treatment of benign prostatic hypertrophy?
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- Tamsulosin
- Alfuzosin - Silodosin |
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What are 4 side effects of using alpha-1 blockers?
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- First dose effect: feel faint
- Nasal congestion - Increase congestive heart failure - Nightmares |
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What drug is a non-selective Beta-1 and Beta-2 receptor blocker?
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- Propanolol
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What are the 12 selective Beta-blockers?
|
- Metoprolol
- Nadolol - Atenolol - Timolol - Esmolol - Betaxolol - Bisoprolol - Pindolol - Penbutolol - Acebutolol - Sotalol - Nebivolol |
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What are 2 antihypertensive drugs that are alpha-1, beta-1 and beta-2 blockers?
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- Labetalol
- Carvedilol |
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What are the 6 Angiotensin Receptor Blockers (ARBs)?
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- Losartan
- Irbesartan - Valsartan - Candesartan - Telmisartan - Eprosartan |
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What do ALL Angiotensin Receptors Blockers cause - what's 1 side effect?
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- Fetal abnormalities
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What does an FDA Category A mean for pregnant women?
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- No risk
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What does an FDA Category B mean for pregnant women?
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- No evidence of risk
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What does an FDA Category C mean for pregnant women?
|
- Risk can't be ruled out because humans have not been tested, but benefits outway risks
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What does an FDA Category D mean for pregnant women?
|
- Evidence of risk to the fetus, but risks = benefits
- Have to make a judgement call |
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What does an FDA Category X mean for pregnant women?
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- Contraindicated use
- Risks are greater than benefits |
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What are the 2 anti-hypertensive drugs that are endothelin blockers?
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- Bosentan
- Ambrisentan |
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What anti-hypertensive drug acts directly on smooth muscle causing K+ channels to open? It is now used as Rogaine.
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- Minoxidil
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What anti-hypertensive drug acts directly on arteries and arterioles causing direct vasodilation? It is almost always administered with a Beta-blocker as well.
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- Hydralazine
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What anti-hypertensive drug acts directly on smooth muscle causing K+ channels to open and can decrease insulin secretion?
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- Diazoxide
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What anti-hypertensive drug is used in hypertensive emergencies and can cause cyanide poisoning if let the mixture sit out too long?
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- Nitroprusside
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What 3 anti-hypertensive drugs are calcium channel blockers?
|
- Nifedipine
- Nicardipine - Amlodipine |
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What are the 7 Angiotensin Converting Enzyme Inhibitors (ACE inhibitors)?
|
- Captopril
- Lisinopril - Fosinopril - Benzapril - Quinapril - Ramipril - Enalapril |
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What anti-hypertensive drug is a renin inhibitor?
|
- Aliskiren
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What anti-hypertensive drug activates D1 receptors?
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- Fenoldopam
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