Exam I: Therapeutic Classification Flashcards
Why are drugs put into Chemical classes (categorized)?
- Structural similarities and moiety (common structural groups)
- Usually similar mechanisms of action
Examples of the potentially different properties of the drug due to structural differences? (7)
- Bioavailability
- Pharmacokinetics: Onset of action
- Duration of activity: The ADR profiles, how long it lasts
- The potency on a weight normalized bases (mg/kg dose)
- Solubility
- Chemical stability
- Patient adherence (palatability)
Benzodiazepines
Central nervous system (CNS) depression and that are most commonly used to treat insomnia and anxiety
Thiazolidinediones
Mostly used to treat type II diabetes
Beta-Lactams
Class of antibiotics
Corticosteroids
Powerful anti-inflammatory drugs, also used for immunosuppressive properties
Aminoglycosides
Antibiotics (differ from beta-lactams), concentration dependent antibiotics that generally kill gram negative organisms
Bisphosphonates
Prevent the loss of bone density, used to treat osteoporosis and similar diseases
Tetracyclines
Antibiotics that may be used to treat infections caused by susceptible microorganisms such as gram positive and gram-negative bacteria, chlamydia, mycoplasma, protozoans, or rickettsia
Proteins (Biotech drug class)
Use biotechnology as a means for manufacturing, which involves the manipulation of microorganisms, such as bacteria, or biological substances, like enzymes, to perform a specific process.
Sulfonamides
Synthetic antibiotic, sulfa drugs
Consoles
Calcium channel blocker, prescribed for high blood pressure and chest pain.
It widens blood vessels and improves blood flow by not making the heart pump harder. It widens blood vessels and improves blood flow
Opioids drug class
Contain chemicals that relax the body and can relieve pain.
Thiazides
Type of diuretic (a drug that increases urine flow).
They act directly on the kidneys and promote diuresis (urine flow) by inhibiting the sodium/chloride cotransporter located in the distal convoluted tubule of a nephron (the functional unit of a kidney).
Barbiturates
Any of a class of sedative and sleep-inducing drugs derived from barbituric acid
Sulfonylureas (ex. glimepiride)
Used to treat type II diabetes by increasing the release of insulin from the pancreas
Monoclonal Antibodies (Biologicals)
Laboratory-produced molecules engineered to serve as substitute antibodies that can restore, enhance, or mimic the immune system’s attack on cancer cells.
Bind to antigens that are generally more numerous on the surface of cancer cells
Thienopyridines (ex. Clopidogrel (Plavix))
Act as a P2Y12 receptor blocker resulting in the inhibition of platelet aggregation
Statins
HMG-CoA reductase inhibitors, are a class of lipid-lowering medications that lower cholesterol levels in the blood to help prevent stroke or heart attack
Why are drugs put into Pharmacological classes?
Have the same pharmacological mode of action
In what ways can drugs in a pharmacological group be the same in relation to their pharmacological mode of action? (Give an example for each)
- Anatomical – CNS drugs, referring to how or where they work a part of the anatomy
- Physiological – CNS depressant, the function is due to the anatomical structure
- Biochemical – Enzyme inducer or inhibitor, how the drug affects an enzyme of the body
- Genetic – Altering the expression of a gene, transfer of genetic material to proteins that can lead to protein synthesis
ACE inhibitors
Relax your veins and arteries to lower your blood pressure by preventing an enzyme in your body from producing angiotensin II, a substance that narrows your blood vessels.
Beta Blockers
Reduce your blood pressure by blocking the effects of the hormone epinephrine, also known as adrenaline.
Beta blockers cause your heart to beat more slowly and with less force, which lowers blood pressure.
Proton Pump Inhibitors
Profound and prolonged reduction of stomach acid production.
Histamine Receptor Antagonists
(H2 blockers) reduce the amount of acid produced by the cells in the lining of the stomach.
Vitamin K Antagonists
Reduce blood clotting by reducing the action of vitamin K
Direct Factor Xa Inhibitors
Direct Thrombin Inhibitors:
Oral agents, have been developed as alternatives to warfarin.
Neuromuscular blocking agents
Drugs that interrupt transmission of nerve impulses at the skeletal neuromuscular junction.
Prevent acetylcholine from triggering the muscle contraction and they are used as anesthesia adjuvants, as relaxants during electroshock, in convulsive states, etc
HMG CoA Reductase Inhibitors
Block an enzyme called HMG-CoA reductase that is involved in the synthesis of mevalonate, a naturally occurring substance that is then used by the body to make sterols, including cholesterol.
PCSK9 Inhibitors
Lower LDL, or “bad,” cholesterol
Angiotensin Receptor Blockers
Medicines that dilate (widen) blood vessels, and are used in the treatment of conditions such as high blood pressure (hypertension), heart failure, or kidney disease in people with diabetes.
How are drugs grouped within Therapeutic classes?
Therapeutic Class is based on the FDA’s approved indications for the majority of drugs in the class
Do not reflect off label uses
Local Anesthetics
Creates an absence of pain in a specific location of the body without a loss of consciousness, as opposed to a general anesthetic
Systemic Anti-infectives
Inhibiting the spread of an infectious organism or by killing the infectious organism outright – anything from antimicrobials to antifungals
Anti-dyslipidemia
Any drug that counters dyslipidemia: abnormal amount of lipids (triglycerides, cholesterol and/or fat phospholipids) in blood
Expectorants
Aid in the clearance of mucus from the upper and lower airways, make coughing easier
Antidepressants
Treat major depressive disorder, some anxiety disorders, some chronic pain conditions, and to help manage some addictions
Anticonvulsants
Treatment of epileptic seizures, also increasingly being used in the treatment of bipolar disorder and borderline personality disorder, since many seem to act as mood stabilizers, and for the treatment of neuropathic pain
Antineoplastic Agents
Used to treat cancer
Antipsychotic Agents
Neuroleptics, are a class of medication primarily used to manage psychosis, principally in schizophrenia but also in a range of other psychotic disorders
Diuretics
Promotes diuresis, the increased production of urine
Hypnotics
Soporific drugs, or “sleeping pills”,
Class of psychoactive drugs whose primary function is to induce sleep and for the treatment of insomnia, or for surgical anesthesia
Anti-inflammatory
Reduces pain, decreases fever, prevents blood clots, and in higher doses, decreases inflammation
What is therapeutic interchange?
The practice of replacing, with the prescribing physician’s approval, a prescription medication originally prescribed for a patient with a chemically different medication
Factors to consider before a therapeutic interchange.
- Must be in the same therapeutic class **
- Consider patient allergies
- Bioavailability (ie. Levothyroxine cannot be interchanged with brand)
- ADME
- Ensure the differences between two medications are not clinically significant
- Cost
- “Generation” - it is assumed that newer drugs have greater safety and efficacy than older drugs
Give an example of a therapeutic drug class that has improved in new generations.
Oral Antipsychotic Drugs
Suffix of 1st gen and 2nd gen antipsychotic drugs.
- azine : First generation
- apine : First or second generation
- piprazole : Second generation
- idone : Second generation
Haloperidol. 1st or 2nd gen antipsychotic?
1st gen
Chlorpromazine. 1st or 2nd gen antipsychotic?
1st gen
Thiothixine. 1st or 2nd gen antipsychotic?
1st gen
Loxapine. 1st or 2nd gen antipsychotic?
1st gen
Only first gen -apine from the list provided
Aripiprazole. 1st or 2nd gen antipsychotic?
2nd gen
Clozapine. 1st or 2nd gen antipsychotic?
2nd gen
Risperidone. 1st or 2nd gen antipsychotic?
2nd gen
What does USAN stand for? What is it?
The United States Adopted Names (USAN) Council is responsible for selecting simple, informative and unique nonproprietary (generic) drug names.
What is the organization that established NDC codes?
USAN council
What are the FDA pregnancy classifications?
A - No risk, human studies
B - No risk, animal studies
C - Risk, Animal studies
D - Risk, Human studies
X - Fetal abnormalities, Animal and Human studies (Do not use in Pregnant Woman)
“Dronate” drugs. Chemical class, Pharmacological class. Therapeutic class.
Chemical class: Bisphosphonates
Pharmacological class: Bone reabsorption inhibitors inhibits the loss of bone structure that occurs over time from “wear & tear.”
Therapeutic Class: Osteoporosis, Heterotropic ossification, Hypercalcemia of malignancy, Paget’s Disease (Osteitis deformans)
May need to know medications prescribed for each indication of “dronate” drugs
See notes. Page 7
What is osteoporosis?
A systemic bone condition characterized by decreased bone mass and deterioration leading to increased bone fragility and risk of hip, spine and wrist fracture
Ratio of females to male that get osteoporosis.
Females 80:20 males
Risk factors for osteoporosis?
- Age: 45+ y/o
- Gender: 4x more likely in women
- Smoker
- Family History
- Nutrition abnormalities: Ca++ and Vitamin D deficiency
- Race: Caucasians and Asians are more susceptible
How common is osteoporosis? What is the extent of the problem?
Affects 200 million globally, 54 million in US
Often asymptomatic until a fracture occurs
What is the role of Ca++ and Vitamin D in Osteoporosis?
- Vit D is needed for calcium absorption
- Hard to get Vit D from diet alone (esp. in winter with no exposure to sun)
- Supplementation is important; however, too much supplementation can lead to nephrolithiasis (kidney stones)
What types of food are rich in vitamin D or calcium for patient who have or are at risk for osteoporosis?
Salmon, tuna, and milk are rich in Vit D
Dairy products and cheese are rich in calcium
What is the main precaution that should taken when a patient is prescribed a “dronate” drug?
Once initiated, -dronate medications should be continued for 5 years in most cases and 10 years in difficult cases
There should be a drug holiday within that period, a period of time when the drug is not taken because of certain serious adverse drug reactions)
How should “dronate” drugs be taken? Why? (i.e. with or w/o food etc.)
- Food often diminishes the absorption of bisphosphonates
- Must take on an empty stomach and have no food for at least 30 minutes after taken
- Advised to take with 6 oz. of water to minimize GI upset
Pregnancy class for “dronate” drugs except (zolendronic acid)
Category C
Zolendronic Acid - D
What is an alternative pharmacotherapy to “dronate” drugs for osteoporosis? Why are bisphosphonates preferred?
Monoclonal antibody drugs are an alternative. SubQ.
Bisphosphonates are not injections so patient compliance is increases and there is a lesser degree of risk vs benefit for these drugs.
FARIN and PARIN (ARIN) drugs. Chemical class. Pharmacological class. Therapeutic class.
Chemical: WarFARIN; all of the PARIN drugs are polysaccharide-like macromolecular structures of varying molecular weights consisting of glycosaminoglycans
Pharmacological: Coagulation pathway inhibitors; vitamin K antagonists
Therapeutic: Myocardial infarction treatment or prophylaxis, Thromboembolism, Angina, DVT, PE, Venous thromboembolism (DVT + PE = VTE)
All the FARIN and PARIN drugs are administered via injection.
True/False
False
Warfarin (Coumadin) is available po
What labs need to be monitored when prescribing Warfarin?
Titrate dosing using the “International Normalized Ratio” [INR]
It involves measurement of the prothrombin time (PT)
Should be between (2 and 3)
Above 3 - Risk of fatal bleeding if above
Below 2 - Risk of clotting
Advantages of Low Molecular Weight Heparins (LMWH) like enoxaparin sodium (Lovenox) (5)
- Made for outpatient
- Subcutaneously administers – well absorbed
- Have predictable pharmacokinetics
- Longer half life
- Safer in most patient populations
Name some of the low molecular weight heparins.
Delteparin
Enoxaparin
Tinzaparin
Fondaparinux
What are the “XABAN” drugs and Dabigatran?
Newer oral alternatives to Warfarin
Advantages of the newer“XABAN” drugs and Dabigatran
- As effective or more effective than Warfarin
- Faster onset of action
- Less intracranial and GI bleeding
- Do not require INR tests
- Fewer dietary restrictions and DDI
- Less frequent dose adjustments
What is the antidote to an excess warfarin response?
Vitamin K
“GREL” drugs. Chemical class. Pharmacological class. Therapeutic class.
Chemical: Thienopyridine prodrugs - activated by enzymes in the gut wall or liver
Pharmacological: Aggregation Inhibitors. Irreversible inhibitors of platelet aggregation
Therapeutic: Anti-atherothrombotic; oral antiplatelet drugs for use with daily p.o.
Indications for “GREL” drug treatment.
Reduce rate of thrombotic CV events including:
Stent Thrombosis with Acute Coronary Syndrome
Are there any black box warnings for “GREL” drugs? (2)
- Patients should be genetically tested because polymorphisms exist for rate of metabolism
Clopidogrel: Diminished effectiveness in slow metabolizers (30% Asians, 17% White)
- Prasugrel and Ticagrelor: Significant and sometimes fatal bleeding risk
This “GREL” drug is less effective in preventing MI and stent thrombosis. Also has a less risk of bleeding.
Clopidogrel (plavix)
What is a prodrug?
A medication that converts into a pharmacologically active drug inside the body.
Improves ADME
For “GREL” drugs, this is a possible DDI for what two classes of drugs?
PPIs and NSAIDs
“ENTAN” drugs. Chemical class. Pharmacological class. Therapeutic class.
Chemical: Carboxylic acid synthetic organic compounds.
Pharmacological: Endothelin receptor antagonist
Therapeutic: Vasodilator for treatment of Pulmonary Arterial Hypertension (Heart and lung vessels)
“Entan” drugs are administered with what types of drugs and therapies? (4)
Diuretics, warfarin, digoxin and oxygen therapy.
“ENTAN drugs” are in the REMS program. Why?
Due to pregnancy category X