Term
| 1. What is the difference between the non-selective alpha 1 adrenergic antagonists discussed in the HTN lecture and the selective alpha 1 adrenergic antagonists discussed this week? |
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Definition
| The selective class inhibits alpha-1a receptors causing relaxation of the smooth muscles in the bladder neck and prostate thereby improving urinary flow rate and symptoms of BPH. It is more specific to those receptors found in the above places. Seventy percent of the alpha-receptors in the prostate are of the 1a subtype. 1b and 1d subtypes mediate vascular smooth muscle contraction. The selective antagonists have much less effect on these types therefore have less of an effect on blood pressure. |
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Term
| 2. What are the adverse effects of the alpha 1 adrenergic antagonists? |
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Definition
What are specific drug interactions that can occur?
Most common adverse effects include hypotension, dizziness, headache, drowsiness, fatigue, nausea, vomiting, constipation, decreased libido. Alfuzosin has additional adverse effect of potential QT prolongation so drug interactions include increased risk of arrhythmias with combination with other agents that cause QT prolongation. Other drug interactions is further hypotension with other antihypertensive agents. |
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Term
| 3. What is the mechanism of action of the 5 alpha-reductase inhibitors? |
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Definition
Inhibits 5 alpha-reductase enzyme thereby inhibiting the conversion of testosterone to 5-alpha
Dihydrotestosterone (DHT: a more potent androgen that stimulates the development of prostate tissue) |
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Term
| 4. List the contraindications of Proscar® and others in this class. |
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Definition
Pregnancy Category X: pregnant women or those trying to become pregnant should not handle crushed or broken tablets
Contraindicated in children
Men taking 5 a-reductase inhibitors should not donate blood (protection of females who may receive blood); should not donate for 6 months following last dose of dutasteride due to long half-life
Caution in those with liver disease
cancer and genital warts. Those types are # 6,11,16,18. It is given in a three dose series and needs to be given before exposure to the virus in order for antibodies to build. |
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Term
| 5. Discuss the various formulations and mechanism of action of the prostaglandin E1 analogs. |
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Definition
| Prostaglandin E1 analog that causes relaxation of the arteriole smooth muscles in the corpus cavernosum resulting in an erection. Induces erection by relaxing trabecular smooth muscle and dilating cavernosal arteries and their branches; dilation of the cavernosal arteries is accompanied by increased arterial inflow velocity and increased venous outflow resistance. Formulations include a SQ injection and a urethral suppository. |
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Term
| 6. List the drug interactions that can occur with phosphodiesterase inhibitors. |
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Definition
Potentiate action of nitrates resulting in
sudden severe hypotension; caution with emergent use of SL nitroglycerin in patient on this class of meds with chest pain
Levels increased by agents that inhibit CYP 3A4; use starting dose of 25 mg in patients taking these agents (max of 25 mg per 48 hours for patients receiving HIV protease inhibitors)
Levels may be decreased by CYP 3A4 inducers
Increased risk of hypotension with alpha blockers-should not taken within 4 hours of alpha blocker |
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Term
| 7. What are the differences in the mechanism of action of the medications used to treat urinary incontinence? |
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Definition
Oxybutynin-Direct antispasmodic effect on smooth muscle, also has anticholinergic/antimuscarinic activity
Trospium chloride-antispasmotic and antimuscarinic agent-non specific
Tolterodine-antimuscarinic activity-ingibits bladder contractions-much less lipophilic than oxybutynin-therefore less entry into CNS and less side effects
Darifenacin/solifenacin-selective M3 muscarinic receptor antagonist-inhibits contractions of the urinary bladder smooth muscle. |
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Term
| 8. What are the most common adverse effects of the agents to treat urinary incontinence? |
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Definition
CNS: drowsiness, dizziness, flushing, headache (CNS effects more common with oxybutynin, dicyclomine, hyoscyamine)
GI: diarrhea, nausea, constipation, dyspepsia, dry mouth
Decreased sweating (oxybutynin)
Cough, nasal dryness, pharyngitis
CV: palpitations, hypertension
Blurred vision, dry eyes
Most common effects with tolterodine are dry mouth, constipation, headache, dizziness, dyspepsia, dry eyes
These adverse effects are related to the anticholinergic effects of the medications. Other medications with anticholinergic effects are TCAs, antihistamines. |
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Term
| 9. What are some alternative agents to use to treat incontinence? |
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Definition
Pseudoephedrine (antihistamines)
Vaginal estrogen ring or creams |
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Term
| 10. What is the difference between active and passive immunity? |
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Definition
| Active immunity occurs when the actual virus or toxin is introduced into the body. This can occur with the administration of a vaccine or by contracting the disease as in chickenpox (acquired immunity). Passive immunity occurs when the actual antibodies are passed to the host. An example of this is during breastfeeding. The mother’s antibodies are passed to the baby and protect them for some time. |
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Term
| 11. What is difference between the live vaccines and the inactivated vaccines? |
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Definition
| Live vaccines have a weakened strain of the actual live virus contained in the formulation. This causes the body to think the disease is occurring in the body. The body then forms antibodies to the virus. With the administration of the live vaccines, side effects may include a mild case of that disease. |
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Term
| 12. In what conditions are the live vaccines contraindicated? |
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Definition
| They are contraindicated with any condition where immunosupression is present. They are also contraindicated in pregnant women. |
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Term
| 13. What is the difference between the two types of pneumococcal vaccines? |
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Definition
| Pneumovax 23® is a 23 valent vaccine and Prevnar® is a 13 valent vaccine. This means that Pneumovax 23® protects against 23 strains of the bacteria and Prevnar® against 13 strains. This Prevnar® 13 replaces Prevnar® 7. Pneumovax 23® is give to patients over the age of 2. Also, Prevnar is a conjugated vaccine. It was noted that there was less immunogenicity in children so Prevnar® was formulated. Its pneumococcal portion is attached to a protein that allows for it to offer more immunoprotective effects. |
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Term
| 14. What is the difference in the two types of polio vaccines? Why was the oral polio vaccine taken off the market? |
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Definition
| The oral polio vaccine was a live virus vaccine. It was found that this vaccine was causing a rise in the occurrences of polio. When the oral polio vaccine is administered, the virus is shed in the feces. Immunocompromised persons that came in contact with these people recently immunized were contracting polio. For this reason the oral formulation was taken off the market. Currently the inactivated formulation is available in an IM injection. |
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Term
| 15. There are several different types of the DTP vaccine. List those types and for which population they are indicated. |
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Definition
| In the past, the formulation DTP was available. This formulation seemed to have many adverse effects associated with it. Because of this DTaP, containing acellular pertussis was introduced. It has been shown to have less adverse effects due to the acellular formulation of the pertussis. Also available is the DT which is used in patients that had an adverse reaction to the DTaP. Td is used in patients over 7 years old and protects against tetanus. Tdap is a new vaccine that has recently been released. It is a booster for those that have completed the 5 dose series before entrance into school. It is given at 11-12 years old. It was released due to the increase in the incidence of pertussis. . |
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Term
| 16. Which of the vaccines are safe to give during pregnancy? |
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Definition
| Hepatitis A and B, IPV, Influenza vaccine (injectable formulation), Td |
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Term
| 17. Who is the influenza vaccine indicated for? What are the contraindications for its use? |
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Definition
| Indicated for those at risk of serious disease or complications (elderly, those with chronic illness, pregnant women, children >6 months old, health care workers, those that do not want to get the flu). The IM formulation is contraindicated in patients with an allergy to eggs and those with an active neurological disorder. The intranasal formulation is contraindicated in those patients that are immunosupressed and pregnant patients due to the fact that it is a live virus formulation. |
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Term
| 18. What are the indications for GardasilÒ? Would you recommend this to your young teenage patients? |
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Definition
| Gardasil® is indicated for females and males ages 9-25 for the treatment of HPV. It covers the high risk virus types that are known to cause cervical |
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Term
| 1. Because phenytoin is highly protein bound, what should you expect with a patient that has a decreased level of albumin? |
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Definition
| A decreased level of albumin does not allow for phenytoin to bind. Those patients that have a decreased level of albumin are at risk for a higher plasma level of phenytoin. This in turn can lead to increased plasma levels of phenytoin which can lead to toxicity. The lab value that will be affected by this is the unbound or free levels of phenytoin. Although this is not routinely checked when checking phenytoin levels, if your patient has a decreased level of albumin and is showing signs of toxicity, you may consider this. |
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Term
| 2. What is true regarding the kinetics of phenytoin? |
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Definition
| It is characterized as having non-linear kinetics. This means that an increase in dose by two-fold may increase the plasma level greater than two fold. Because of this, it is important to obtain levels frequently throughout medication adjustments and titrate the drug upwards slowly. |
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Term
| 3. Give examples of drug interactions with phenytoin due to its involvement in the P450 enzyme system. |
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Definition
Drugs that inhibit the metabolism of phenytoin include (but are not limited to) benzodiazepines, azole antifungals, cimetidine-they are inhibitors of the enzyme. They cause an increase in the plasma levels of phenytoin.
Drugs that increase the metabolism are the inducers of the enzyme system. These include (but are not limited to) barbiturates, carbamazepine, rifampin. This means that there will be a decreased level of phenytoin in plasma.
Because phenytoin is a P450 inducer, it can increase the metabolism of other drugs. Those drugs include (but are not limited to) estrogens (including oral contraceptives), valproic acid, phenothiazines, furosemide, haloperidol. |
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Term
| 4. What adverse effects similarly occur with most anticonvulsants? |
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Definition
| Mainly lethargy, sedation, headache, confusion, ataxia, tremors, mental status changes, GI effects. Others although rare can cause Stevens- Johnson’s syndrome (some), leukopenia (some), thrombocytopenia. |
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Term
| 5. Which neurotransmitters do barbiturates and other anticonvulsants exert their effect? |
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Definition
| GABA-an inhibitory neurotransmitter in the CNS. For the meds that act on GABA, (e.g. phenobarb, valproate, gabapentin), they can potentiate the effects of GABA in different ways: inhibit the enzyme that breaks down GABA, increase binding of GABA to its receptors, or inhibiting the reuptake of GABA. Some agents (e.g. phenytoin, carbamazepine) inhibit neuronal firing by blocking sodium channels. |
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Term
| 6. Why are barbiturates to be used with caution in suicidal patients and those with substance abuse? |
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Definition
| This group of medications can be addicting. Patients can also build up a tolerance to the medication. Also, this group of medications can cause increased sedation in higher doses. Those patients at risk for suicide can easily overdose on these medications. |
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Term
| 7. What effects does administering Gabapentin with antacids have? |
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Definition
| Antacids administered with Gabapentin can decrease the bioavailability of the medication. Gabapentin should be administered 2 hours before or 2 hours after antacid. |
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Term
| 8. What neurotransmitters does lamotrigine exert its effect on? |
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Definition
| It inhibits glutamate and asparatate, two excitatory neurotransmitters found in the CNS. |
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Term
| 9. Which anticonvulsants are not involved in the P450 enzyme system, decreasing the amount of drug interactions that can occur? |
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Definition
Levitiracetam (Keppra®)
Gabapentin |
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Term
| 10. When treating patients with Parkinson’s which neurotransmitter are the medications targeting? |
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Definition
| Therapy for Parkinson’s disease is targeted toward increasing dopamine activity at the receptor site or reducing cholinergic stimulation at the receptor. |
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Term
| 11. What is the importance of the combination of levodopa plus carbidopa? |
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Definition
| Levodopa is rapidly converted to dopamine by dopa-decarboxylase in the periphery and central nervous system. 95% is decarboxylated in the periphery. Levodopa crosses the blood brain barrier and carbidopa does not. Carbidopa increases cerebral concentrations of dopamine by inhibiting peripheral dopa-decarboxylase, preventing the metabolism of levodopa. When administered together, carbidopa prevents the metabolism of levodopa, enabling more levodopa to reach the CNS, exerting its effect. |
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Term
| 12. What interaction can occur with the administration of dopamine antagonists with the medications used to treat Parkinsons? |
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Definition
| Because drugs for the treatment of Parkinson’s disease are dopamine agonists, if given with dopamine antagonists (phenothiazines, metoclopramide), this will antagonize the effects of the medications used for treatment. |
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Term
| 19. How does urine pH affect the levels of memantine? |
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Definition
| This medication is renally excreted. The characteristics of the urine will affect the elimination of this drug. If the urine is acidic, this may increase the elimination of the drug. If the urine is more alkaline, this may decrease the elimination of this drug. |
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Term
| 13. How does selegiline differ from the other medications in its mechanism of action? Why is this significant and what drug/food interactions can be expected? |
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Definition
| Selegiline is an antagonist for MAO type B. This is responsible for the breakdown of dopamine in the CNS. It is more selective than MAOIs used for depression, however, it has the same drug and food interactions. It is contraindicated with MAOI use and any serotonergic medications (SSRIs, tramadol). Also patients taking this drug should decrease the amount of foods containing tyramine to prevent hypertensive crisis. |
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Term
| 14. Of those agents that stimulate dopamine receptors, what are the significant differences in the medications in this class? |
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Definition
The agents that stimulate dopamine receptors are bromocriptine, pergolide, pramipexole and ropinirole.
Drug Receptor Type of drug Pharm. other
bromocriptine Agonist D2
Partial antagonist D1 Ergot alkaloid Poor bioavail
High first pass
CYP3A4 substrate
Half life 3 hrs Also used in hyperprolactinemia-Contraind with breast feeding
pergolide Agonist D1and D2 Ergot Alkaloid Good bioavail
Half life 27 hrs 10x stronger than bromocriptine
pramipexole Binds to D2 and D3 receptors Not ergot Good bioavail.
Half life 8-12 hrs
ropinirole Acts at D2 and D3 receptors Non-ergot Bioavail 55%
Half life 6 hours
Met-CYP1A2 |
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Term
| 15. How does tolcapone differ in its mechanism of action in relationship to the other anitparkinsonian agents? |
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Definition
| Tolcapone exerts its effect on COMT catechol-o-methltransferace. This enzyme is responsible for the breakdown of catecholamines such as dopamine, norepinephrine, epinephrine. This enzyme is the main enzyme responsible for the breakdown of levodopa. The inhibition of COMT, allows for an increased level of levodopa for use in the CNS. This medication is used in conjunction with levodopa/carbidopa allowing for a decrease in dosage of levodopa. |
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Term
| 16. What is the goal of therapy when treating Alzheimer’s disease? |
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Definition
| Maintain and maximize patients functioning, quality of life and help maintain their independence. An important part of treatment of Alzheimers is to have a multidisciplinary approach which includes the family of these patients. |
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Term
| 17. What is the mechanism of action for Donepezil (Aricept) and others in this class? |
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Definition
| This class of medications is also known as cholinesterase inhibitors. They inhibit the enzymes that are responsible for the breakdown of Acetylcholine. There are two types of enzymes that these drugs act upon: Butyrylcholinesterase located in the periphery and acetylcholinesterase located in the CNS. This class of drugs requires that intact cholinergic neurons be present. |
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Term
| 18. What are the clinical differences in these medications in the above class? |
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Definition
Drug Pharm Other
tacrine Met CYP1A2
Short half-live of 1-4 hours
Absorption decreased with food. Liver toxicity-requires frequent drug monitoring Not used as much due to this.
donepezil Met CYP2D6, 3A4
Half life 70hrs Greater affect on acetylcholinesterase centrally located enzyme.
rivastigmine Half life 2hrs but effects last 12 hrs. Renally excreted Caution with renal disease
galantamine Completely absorbed Renally excreted Caution with renal disease. |
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Term
| 1. Which agents are most effective for the treatment of neuropathic pain? |
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Definition
Anticonvulsants (i.e. gabapentin, carbamazepine), tricyclic antidepressants (i.e.
amitriptyline), Lyrica and capsaicin (less effective) |
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Term
| 2. How do the nonacetylated salicylates differ from the acetylated salicylates? |
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Definition
Nonacetylated agents are reversible inhibitors of the COX enzyme and have less
antiplatelet effects and less GI adverse effects. |
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Term
| 3. What are the differences between the COX-2 inhibitors and traditional NSAIDS? |
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Definition
| More selective inhibition of COX-2 versus COX-1 enzyme. Traditional NSAIDS are nonselective inhibitors of COX-1 and COX-2. Less GI adverse effects since COX-2inhibitors do not inhibit COX-1 enzyme found in GI mucosa. Less antiplatelet effects. |
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Term
| 4. Which pain medications should be used with caution with the SSRIs due to increased risk of seizures? |
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Definition
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Term
| 5. What are the contraindications/precautions of the use of opioid analgesics? |
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Definition
Avoid abrupt discontinuation of these agents, withdrawal can be seen
Use cautiously in patients with head injury, increased intracranial pressure,
decreased respiratory reserve (i.e. COPD), supraventricular arrhythmias (question came up as to why this is a precaution-the only reasoning I could find was due to the potential CV effects of bradycardia/hypotension with opiates), prostatic hypertrophy or urethral stricture, elderly or debilitated patients, patients with acute abdominal painTramadol is contraindicated in cases of acute ethanol intoxication and intoxication with other agents such as opiate agonists, hypnotics, centrally acting analgesics, or psychotropic drugs increased risk of seizures when naloxone is used to reverse respiratory depression with tramadol
Pregnancy category C; pregnancy category D when used for prolonged periods or at high doses close to term |
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Term
| 6. Describe some characteristics of meperidine that differentiate it from other opioid analgesics? |
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Definition
Not very effective orally-oral use not recommended
Synthetic agent (can be used in someone with true morphine or codeine allergy
which is extremely rare)
Active metabolite, normeperidine, associated with seizure particularly in patients with renal dysfunction who have an impaired ability to eliminate the metabolite |
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Term
| 7. What are the signs and symptoms of opioid intoxication? |
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Definition
Miosis, drowsiness, decreased rate and depth of respiration, bradycardia,
hypotension |
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Term
| 8. Which of the muscle relaxants is structurally related to the TCAs and therefore has similar adverse effects, contraindications, precautions as the TCAs? |
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Definition
| Cyclobenzaprine (Flexeril) |
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Term
| 9. Which of the muscle relaxants is a centrally acting α-2 agonist that is structurally related to clonidine? |
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Definition
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Term
| 10. What are some contraindications/precautions to the use of “triptans”? |
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Definition
Contraindicated in patients with coronary artery disease, angina, cerebrovascular
disease, peripheral vascular disease, acute myocardial infarction, history of
myocardial infarction, silent myocardial ischemia, Raynaud’s disease, Wolff-
Parkinson-White syndrome, ischemic bowel disease/ischemic colitis, or uncontrolled hypertension.
Caution in patients who have risk factors for CAD (diabetes mellitus, hypertension, hypercholesterolemia, obesity, family history of CAD, tobacco s moking, postmenopausal female, or male > 40 years of age)-cardiac work-up is advised prior to use of triptans in these patients and first-dose should be initiated under medical supervision
Caution in patients with seizure disorderCaution in patients with renal or hepatic impairment
Pregnancy category C |
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Term
| 11. Which agents are most appropriate for prevention of migraine headaches? |
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Definition
| First-line: Propranolol, timolol, amitriptyline, divalproex sodium, sodium valproate, topamax |
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Term
| 12. What are the signs and symptoms of ergot toxicity? |
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Definition
Abdominal pain, anxiety, chest pain, myalgia, severe nausea and vomiting,
numbness, tingling, or vision changes |
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Term
| 13. Which antigout medications are appropriate for treating an acute gouty attack? |
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Definition
NSAIDS (indomethacin usually drug of choice)
Colchicine
Corticosteroids |
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Term
14. Which antigout medications are appropriate for prevention of an acute gouty
attack? |
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Definition
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Term
| 15.Describe the mechanism of action of antigout medications covered in the previous question. |
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Definition
Probenecid: Inhibits tubular reabsorption of uric acid, increasing urinary excretion of uric acid
Allopurinol: Inhibits production of uric acid by inhibiting the enzyme xanthine oxidase which converts hypoxanthine and xanthine to uric acid. |
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