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Lisinopril is the generic form of the brand-name drug Zestril, a medication prescribed to treat high blood pressure.
Doctors also prescribe lisinopril in combination with other drugs to treat congestive heart failure.
Lisinopril is in a class of medications called angiotensin-converting enzyme inhibitors, or ACE inhibitors.
It works by widening blood vessels, which allows blood to flow more smoothly and lets the heart function more efficiently.
By lowering blood pressure, lisinopril also helps reduce the risk for stroke and heart attack.
The Food and Drug Administration (FDA) first approved lisinopril in 1987.
The drug company Merck developed lisinopril under the brand name Prinivil.
In 2002, the FDA approved generic lisinopril.
Lisinopril Warnings If you take medication or insulin to treat diabetes, track your blood sugar carefully while also taking lisinopril, particularly during the first month of its use.
The combination of these diabetes drugs can cause a drop in your blood sugar levels.
It’s also important to be aware of any signs of infection, such as sore throat or fever, which could indicate problems with your white blood cell count.
Before starting on lisinopril, be sure to let your doctor know if you have any type of surgery planned, including dental surgery.
Tell your doctor if you have angioedema, a condition that causes trouble swallowing or breathing as well as painful swelling in various parts of the body, including the face, throat, eyes, hands, feet, ankles, and lower legs.
You should also let your doctor know if you have diabetes and are taking aliskiren (Tekturna, Amturnide, Tekamlo, Tekturna HCT).
Your doctor also needs to know if you’ve ever had: Heart or kidney disease Lupus Scleroderma Pregnancy and Lisinopril There’s strong evidence that lisinopril can harm an unborn baby.
Make sure your doctor knows if you are pregnant, or may become pregnant, before taking lisinopril.
If you get pregnant while taking lisinopril, call your doctor right away.
It’s unknown whether the drug passes into a woman’s breast milk, but to be safe, women who are breastfeeding should stop breastfeeding (or not take lisinopril).
Research shows that lisinopril is safe and effective for children older than 6 and for teenagers.
There’s not enough evidence to say that it’s safe for younger children.
BasicDescription Back to Top Lisinopril Side Effects Common side effects of lisinopril include: Cough Dizziness Headache Extreme tiredness Nausea Diarrhea Weakness Sneezing Runny nose Low sex drive Rash Serious side effects can also occur.
If you have any of these side effects, call your doctor right away: Swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs Hoarseness Trouble breathing or swallowing Signs of infection, such as fever, sore throat, and chills Yellowing of the skin or eyes Lightheadedness or fainting Chest pain Back to Top Lisinopril Interactions Some drugs may affect the way lisinopril works, and lisinopril could also affect other medications.
It’s very important to let your doctor know about everything you are taking, including any over-the-counter (OTC) medications, herbs, or supplements as well as illegal drugs.
Drugs that interact with lisinopril include: Aspirin and other non-steroidal anti-inflammatory drugs (NSAIDs ), such as indomethacin (Indocin) Diuretics (“water pills”) Potassium supplements Medications for diabetes, such as insulin and aliskiren (Tekturna, Amturnide, Tekamlo, Tekturna HCT) The antidepressant lithium (Eskalith, Lithobid) Other ACE inhibitors Lisinopril and Alcohol People taking lisinopril are advised to avoid drinking alcohol.
Alcohol can also lower your blood pressure, and may increase your risk of certain side effects of lisinopril.
Other Lisinopril Interactions It’s important to talk to your doctor before using any salt substitutes that contain potassium when you’re taking lisinopril.
Your doctor may also tell you to follow a low-salt or low-sodium diet.
It’s important to follow these directions carefully.
Back to Top Lisinopril Dosage Lisinopril is a tablet that you take orally.
It’s available in various strengths, ranging from 2.5 milligrams (mg) to 40 mg.
You’ll typically take lisinopril once a day, around the same time each day.
Your doctor will probably prescribe a low dose of the drug at first and gradually increase it over time.
For people with high blood pressure, the typical dose of lisinopril ranges from 20 to 40 mg a day.
When treating heart failure, the effective dose of the drug ranges from 5 to 40 mg a day.
For people who’ve had a heart attack, the first dose of lisinopril is 5 mg.
After 24 hours, you’ll take another 5 mg.
After 48 hours, you’ll take 10 mg a day for six weeks.
For children, the usual starting dose of lisinopril is up to 5 mg daily.
Lisinopril Overdose Taking too much lisinopril would most likely lead to low blood pressure.
Symptoms of a lisinopril overdose could include: Lightheadedness Fainting If you or someone else has symptoms of an overdose, call a poison control center at 1-800-222-1222.
If someone collapses or isn’t breathing, call 911.
Missed Dose of Lisinopril Keep taking lisinopril, even if you feel well.
Don’t stop taking lisinopril without talking to your doctor first.
If you miss a dose of lisinopril, take the missed dose as soon as you remember it.
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Ezetimibe is a drug that lowers plasma cholesterol levels. It acts by decreasing cholesterol absorption in the small intestine. It may be used alone (marketed as Zetia or Ezetrol ), when other cholesterol-lowering medications are not tolerated, or together with statins (e.g., ezetimibe/simvastatin, marketed as Vytorin or Inegy ) when statins alone do not control cholesterol.
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Contents
1 Medical uses
2 Contraindications
3 Adverse effects
4 Overdose
5 Mechanism of action
6 Pharmacokinetics
7 See also
8 References
Medical uses
As of mid-2014, treatment guidelines of the American Heart Association /American College of Cardiology recommend ezetimibe as one of several second line treatment options for people who are intolerant of statins or who are unable to reach serum LDL goals using statins alone.
While ezetimibe reduces LDL cholesterol, it has not been shown to affect outcomes such as risk of death or major cardiovascular event like heart attack or stroke.
Ezetimibe is indicated in the United States as an add-on to dietary measures to:
reduce levels of certain lipids in people with primary hyperlipidemia, alone or with a statin ;
reduce levels of certain lipids in people with mixed hyperlipidemia, in combination with fenofibrate ;
reduce levels of certain lipids in people with homozygous familial hypercholesterolemia, in combination with specific statins;
reduce levels of certain lipids in people with homozygous sitosterolemia.
Contraindications
The two contraindications to taking ezetimibe are a previous allergic reaction to ezetimibe, including symptoms of rash, angioedema, and anaphylaxis, and severe liver disease, especially when taken with a statin.
Ezetimibe may have significant medication interactions with cyclosporine and with fibrates other than fenofibrate.
Adverse effects
Common adverse drug reactions (≥1% of patients) associated with ezetimibe therapy include: headache and/or diarrhea (steatorrhea). Infrequent adverse effects (0.1–1% of patients) include: myalgia and/or raised liver function test ( ALT / AST ) results. Rarely (<0.1% of patients), hypersensitivity reactions (rash, angioedema ) or myopathy may occur. Overdose The incidence of overdose with ezetimibe is rare; there is subsequently little data on the effects of overdose. However, an acute overdose of ezetimibe is expected to produce an exaggeration of its usual effects, leading to loose stools, abdominal pain, and fatigue. Mechanism of action Ezetimibe inhibits the absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver cells, leading them to absorb more from circulation and thus lowering levels of circulating cholesterol. The exact mechanism is not known, but it appears that ezetimibe blocks the critical mediator of cholesterol absorption, the Niemann-Pick C1-like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes ; blocks aminopeptidase N, and interrupts a Caveolin 1 - Annexin A2 complex involved in trafficking cholesterol. Pharmacokinetics Within 4–12 hours of the oral administration of a 10 mg dose to fasting adults, the attained mean ezetimibe peak plasma concentration ( C max ) was 3.4–5.5 ng/ml. Following oral administration, ezetimibe is absorbed and extensively conjugated to a phenolic glucuronide (active metabolite). Mean C max (45–71 ng/ml) of ezetimibe-glucuronide is attained within 1–2 h. The concomitant administration of food (high-fat vs. nonfat meals) has no effect on the extent of absorption of ezetimibe. However, coadministration with a high-fat meal increases the C max of ezetimibe by 38%. The absolute bioavailability cannot be determined, since ezetimibe is insoluble in aqueous media suitable for injection. Ezetimibe and its active metabolite are highly bound to human plasma proteins (90%). Ezetimibe is primarily metabolized in the liver and the small intestine via glucuronide conjugation with subsequent renal and biliary excretion. See also Cholesterol absorption inhibitor Ezetimibe/simvastatin Ezetimibe/atorvastatin Niacin SCH-48461 NPC1L1

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Prazosin, sold under the brand name Minipress, is a prescription medication used to treat high blood pressure.
The drug may also be used to treat patients with an enlarged prostate, congestive heart failure, Raynaud’s disease, pheochromocytoma, and Ergot alkaloid poisoning.
Some doctors prescribe prazosin to people with post-traumatic stress disorder, as it blocks the body’s release of the hormone adrenaline.
Prazosin is one drug in the class of alpha-adrenergic blockers, which work by relaxing the blood vessels so that blood can pass through more easily.
Prazosin comes in a tablet and capsule form and is manufactured by Pfizer, Inc.
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This effect usually stops once your body gets used to the medication.
Try not to stand up too quickly.
Older patients may be more sensitive to the side effects of prazosin, especially dizziness and fainting, which can increase the risk of falling.
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The drug passes through breast milk.
BasicDescription Back to Top Prazosin Side Effects Common Side Effects of Prazosin: Some less serious side effects of prazosin include: Weakness Tiredness Dizziness Nausea Serious Side Effects of Prazosin: You should call your doctor if you experience any of the following serious side effects: Fast or pounding heartbeat or fluttering in your chest Feeling like you might pass out Trouble breathing Swelling in the hands, ankles, or feet An erection that is painful or lasts four or more hours Back to Top Prazosin Interactions Prazosin and Other Drug Interactions Some drugs that may interact with prazosin include: Beta blockers, such as atenolol (Tenormin), metoprolol (Toprol-XL), propranolol ( Inderal ) Verapamil (Calan) Erectile dysfunction or pulmonary hypertension meds Antihistamines, such as diphenhydramine (llermax, Banophen, Benadryl ) Anti-seizure drugs, such as carbamazepine (Carbatrol, Epitol, Equetro, Tegretol ) Drugs for sleep or anxiety, such as alprazolam (Niravam, Xanax, Xanax XR), diazepam (Valium), zolpidem (Ambien) Muscle relaxants Narcotic pain relievers (such as codeine ) Psychiatric meds, such as chlorpromazine ( Thorazine ), risperidone (Risperdal), amitriptyline (Elavil), trazodone (Desyrel) Check the labels on all of your medications because they may contain ingredients that can increase your blood pressure or cause a fast heartbeat.
This drug may also interfere with certain lab tests, so you should tell laboratory personnel you are taking prazosin.
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Prazosin and Other Interactions This drug may impair your vision and make you dizzy or drowsy.
Do not drive, use machinery, or perform any other activity that requires alertness until you are sure you can do so safely.
You should also limit your alcohol intake while taking prazosin.
Back to Top Prazosin Dosage The amount of prazosin you take will depend on your doctor’s instructions.
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Then, your doctor will slowly increase your dose to 6-15 mg, divided into two or three doses a day.
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This is typically divided into two or three doses.
Prazosin Overdose If you suspect an overdose, contact a poison control center at (800) 222-1222 or an emergency room immediately.
Missed Prazosin If you miss a dose of prazosin, take it as soon as you remember.
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Theophylline is the generic name for the prescription drugs Uniphyl (in Canada) and Theo-24.
It’s used to treat airflow obstruction symptoms such as wheezing, shortness of breath, and chest tightness related to asthma and lung diseases, including emphysema and chronic bronchitis.
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Theophylline may be prescribed off-label to treat sleep apnea or asthma attacks that aren’t responding to other treatments.
It’s also sometimes used for breathing problems in premature infants.
The Food and Drug Administration first approved Uniphyl theophylline (produced by Purdue Pharma) in 1982, and Theo-24 (UCB Inc.) in 1983.
Theophylline Warnings You should not use theophylline if you’re hypersensitive to the drug or its components.
Theophylline can also worsen some conditions, so you shouldn’t use it if you have: Ulcers Seizure disorders Some forms of cardiac arrhythmias (abnormal heart rate) Under certain conditions, the drug can remain in your body longer than normal and build up to unsafe levels, resulting in fatal toxic reactions.
In these cases, you should not take theophylline unless the benefits clearly outweigh the risk, and then your doctor will have to carefully decide on your dosage and monitor your blood for levels of the drug.
The conditions that can lead to a deadly toxic reaction include: Being younger than 1 year old, or older than 60 years Congestive heart failure and right-sided heart failure (cor pulmonale) that typically arises from high blood pressure A buildup of fluid in the lungs (acute pulmonary edema) Liver disease, acute hepatitis, or cirrhosis (scarring of the liver) Reduced kidney function Cystic fibrosis A fever of 102 Fahrenheit or more that lasts 24 hours, or a low fever that lasts longer than a day A high- carbohydrate, low-protein diet Thyroid disease A state of physical shutdown called shock Sepsis (blood infection) with multi-organ failure The flu Tobacco and marijuana smoking Stopping smoking Taking or stopping certain drugs while on theophylline You need to be very careful about other drugs you are on or stop taking because of the same potentially fatal toxic reaction.
Pregnancy and Theophylline Theophylline is an FDA Pregnancy Category C drug, meaning that a possible risk to developing fetuses cannot be ruled out.
Studies in animals have shown that the drug can cause birth defects, but no adequate and well-controlled studies have been conducted in pregnant women.
Theophylline should only be used during pregnancy if the potential benefits to the mother outweigh the risks to her unborn child.
Theophylline is excreted in breast milk, potentially causing irritability and other signs of mild toxicity in breastfeeding infants.
It’s not likely to cause serious side effects in infants unless the breastfeeding mother has very high concentrations of the drug in her body.
Nonetheless, if you are breastfeeding your child, you shouldn’t take theophylline unless the potential benefits outweigh the risks, and then only under the guidance of your doctor.
Theophylline for Dogs and Cats The FDA has not approved theophylline for veterinary medicine, but it is commonly prescribed to treat heart failure, asthma, pulmonary edema, bronchitis, and chronic obstructive pulmonary disease in cats and dogs.
As with people, pets are more likely to experience issues with theophylline if they have certain health conditions or are also taking other medications.
Potential side effects include restlessness, upset stomach, frequent urination, and rapid heartbeat.
Always talk to your pet’s veterinarian before giving your dog or cat any prescription drug, including theophylline.
BasicDescription Back to Top Theophylline Side Effects Common Side Effects of Theophylline Although these effects are common, they can be serious and are likely to mean your doctor should change your dosage.
Tell your doctor if you experience any of the following, and if the effect becomes severe, get immediate medical help: Nausea and vomiting Headache Upset stomach Loss of appetite Fast, strong heartbeat Irregular heartbeat ( arrhythmia ): usually there are no symptoms, but it can cause a fluttering feeling, dizziness, shortness of breath, chest pain, heartbeats that feel too fast or slow, or fainting Symptoms similar to how you feel when you’ve had too much coffee, such as trouble falling asleep (insomnia), restlessness, and irritability.
Skin rash Severe Side Effects of Theophylline You need immediate emergency medical treatment if you are experiencing: Seizures Rare Side Effects of Theophylline Tell your doctor right away or get emergency medical help if you experience any of the following more rare side effects: Stomach pain Anxiety Diarrhea Dizziness Tremors Urination issues, including frequent or infrequent urination and hyperuricemia (high levels of uric acid) Allergic reaction Reflux Back to Top Theophylline Interactions Some drugs can affect your body’s ability to process theophylline, potentially causing it to build up to unsafe levels and become toxic.
In addition, theophylline interacts with a wide variety of other drugs, so it’s especially important to tell your doctor about any medications, illegal or recreational drugs, herbal remedies, and supplements you’re taking, even if you are smoking tobacco.
The following drugs are especially important to tell your doctor about before you take theophylline: Adenosine (Adenoscan) Allopurinol (Zyloprim) Aminoglutethimide (Cytadren) Carbamazepine ( Tegretol ) Cimetidine Ciprofloxacin (Cipro) Clarithromycin (Biaxin) Diazepam (Valium) Disulfiram ( Antabuse ) Enoxacin Ephedrine Erythromycin (Ery-tab) Estrogen -containing oral contraceptives Flurazepam (Dalmane) Fluvoxamine ( Luvox ) Halothane (Fluothane) Interferon Isoproterenol (Isuprel) Ketamine (Ketalar) Lithium Lorazepam (Ativan) Methotrexate ( Trexall ) Mexiletine (Mexitil) Midazolam Moricizine Pancuronium (Pavulon) Pentoxifylline (Trenal) Phenobarbital Phenytoin ( Dilantin ) Propafenone (Rythmol) Propranolol ( Inderal ) Rifampin (Rifadin) Ritonavir Roflumilast (Daliresp) St.
John’s wort Sulfinpyrazone (Anturane) Tacrine (Cognex) Thiabendazole (Mintezol) Ticlopidine (Ticlid) Troleandomycin (Tao) Verapamil (Calan) Theophylline and Alcohol Drinking alcohol while taking theophylline may cause the drug to remain in your body for up to 30 percent longer, which can lead to serious toxic effects.
Therefore, you should not drink alcohol when taking theophylline.
Back to Top Theophylline Dosage Your doctor may start you on a low dose of theophylline then gradually increase it while monitoring your symptoms and blood levels for the drug.
Theophylline (Uniphyl and Theo-24) comes as controlled-release tablets, which are generally taken once a day with food or within one to two hours of mealtime.
Theophylline also can be taken multiple times per day in an oral solution form.
Tablets must be swallowed whole.
You must not chew, split, or crush them.
Theophylline Overdose A sudden overdose from taking too much theophylline all at once is rare.
A chronic overdose, however, is not rare, especially if you have been taking a dose that is a little too high for a long time, or if your dose has recently been increased.
An overdose of theophylline may cause slow heart rate, abnormal heart rate, seizures, circulatory system failure, and death.
If you suspect an overdose, you should contact a poison-control center or emergency room immediately.
You can reach a poison-control center at (800) 222-1222.
Missed Dose of Theophylline Missing a dose of theophylline may cause your asthma or bronchitis symptoms to reappear.
If you remember your missed dose within 6 hours of your regular dosing time, take your missed dose immediately.
Take half a dose if you remember the missed dose between 6 and 18 hours after your regular time.
If more than 18 hours have passed since your missed dose, skip it and take your next dose at your regular dosing time.
Never double-up a dose of theophylline.
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Leflunomide is the generic form of the brand-name medicine Arava, which is used to treat rheumatoid arthritis (a condition in which the body attacks its own joints).
This prescription medication is also sometimes used to help treat psoriatic arthritis (a condition that causes joint pain and scaly skin).
Leflunomide belongs to a class of drugs called disease-modifying antirheumatic drugs (DMARDs).
It works by suppressing blood cells that cause inflammation.
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Leflunomide Warnings Leflunomide contains a black box warning because it may cause serious liver problems that could potentially lead to death.
Tell your doctor immediately if you experience any of the following symptoms while taking this medicine: Yellowing of the skin or eyes ( jaundice ) Dark-colored urine Pale-colored stools Pain in the upper right part of the stomach Severe or persistent nausea Loss of appetite Extreme tiredness Unusual bleeding or bruising Your doctor will monitor your liver function carefully while you take this medicine.
Don’t take leflunomide if you have any type of liver problem.
Drinking alcohol while you’re on leflunomide may increase the risk of liver complications.
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Also, tell your doctor if you’re taking any of the following medicines before starting on leflunomide: Tylenol (acetaminophen) Aspirin and other nonsteroidal anti-inflammatory drugs ( NSAIDs ), such as Advil or Motrin ( ibuprofen ) and Aleve or Naprosyn ( naproxen ) Cholesterol -lowering medications ( statins ) Hydroxychloroquine Iron products Laniazid, Rifamate, or Rifater ( isoniazid ) Trexall (methotrexate) Niacin Rifadin, Rimactane, Rifamate, or Rifater ( rifampin ) Leflunomide may lower your body’s ability to fight infections.
Tell your doctor right away if you experience any of the following symptoms while taking this medicine: Fever Sore throat Cough Flu -like symptoms Red, warm, swollen, or painful skin Difficult, painful, or frequent urination Don’t receive any vaccines while taking leflunomide without first discussing it with your doctor.
Tell your doctor if you’re prone to getting infections or if you currently have an infection.
It’s possible that you could have tuberculosis (TB — a serious lung infection) and not know it.
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Tell your doctor if you have or have ever had TB, have been around someone with TB, or have traveled to areas where TB is common.
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Your healthcare provider will probably want to check your blood pressure before you start on the drug, and frequently throughout your treatment.
Leflunomide may cause birth defects and other serious problems in the offspring of both women and men.
This medicine can stay in your body for up to two years after you stop taking it.
Both women and men who use leflunomide should use effective forms of birth control to prevent pregnancy for as long as your doctor recommends.
If you’re a man who wants to father a child, talk to your doctor about stopping leflunomide and receiving a therapy that helps remove the medicine from your body more quickly.
Pregnancy and Leflunomide Leflunomide contains a black box warning because it could harm an unborn baby.
Don’t take this medicine if you’re pregnant or plan to become pregnant.
You’ll need to use an effective form of birth control before taking leflunomide, during your treatment, and for two years after your treatment ends.
Call your doctor immediately if you think you might be pregnant while using leflunomide.
Let your doctor know if you want to become pregnant within two years of stopping this medicine.
Your healthcare provider may prescribe a treatment that can remove this drug from your body more quickly.
It’s not known whether leflunomide passes into breastmilk or could hurt a breastfeeding baby.
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BasicDescription Back to Top Leflunomide Side Effects Common Side Effects of Leflunomide Tell your doctor if any of the following side effects become severe or don’t go away: Diarrhea Vomiting Heartburn Headache Runny nose Dizziness Weight loss Mild muscle aches Back pain Dry skin Hair loss Serious Side Effects of Leflunomide Tell your doctor immediately if you experience any of the symptoms listed in the Leflunomide Warnings section above, or any of the following serious side effects: A rash with or without a fever Mouth sores Itching Blisters on the skin, eyes, or nose Peeling of the skin Chest pain Fast or irregular heartbeat Pale skin New or worsening cough Leg cramps Muscle pain or weakness Pain, burning, numbness, or tingling in the hands or feet Severe or persistent vomiting Severe or persistent headache or dizziness Vision changes Signs of a severe allergic reaction (may include hives, difficulty breathing, tightness in the chest, or swelling of the mouth, face, lips, or tongue) Back to Top Leflunomide Interactions Tell your doctor about all prescription, non-prescription, illegal, recreational, herbal, nutritional, or dietary drugs you’re taking, especially those listed in the Leflunomide Warnings section above, and any of the following: Blood thinners, such as Coumadin (warfarin) Prevalite ( cholestyramine ) Gold compounds, such as Ridaura (auranofin) Medications to treat cancer Other medications that suppress the immune system, such as Azasan or Imuran ( azathioprine ), Gengraf, Neoral, or Sandimmune ( cyclosporine ), Rapamune (sirolimus), and Astagraf or Prograf ( tacrolimus ) Cuprimine or Depen (penicillamine) Tolbutamide Leflunomide and Other Interactions Leflunomide can cause dizziness.
Don’t drive, operate machinery, or perform any task that requires alertness until you know how this medicine affects you.
Leflunomide and Alcohol Drinking alcohol while taking leflunomide can worsen certain side effects and increase your risk of developing liver problems.
Talk to your doctor before consuming alcoholic beverages while using this medicine.
Back to Top Leflunomide Dosage Leflunomide comes as a tablet to take by mouth, typically once a day.
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Your doctor may start you on a higher dose of leflunomide for the first few days of treatment.
Follow the instructions or your prescription label carefully when taking this medicine.
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It could take four weeks or longer before you notice the benefits of leflunomide.
Continue to take this medicine even if you feel well.
Don’t stop using it without first talking with your doctor.
Leflunomide Overdose Symptoms of a leflunomide overdose may include: Stomach pain Diarrhea Weakness Extreme tiredness Pale skin Shortness of breath Fast heartbeat If you suspect an overdose, contact a poison control center or emergency room immediately.
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Missed Dose of Leflunomide If you miss a dose of leflunomide, take it as soon as you remember.
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Additional information about the drug Efavirenz


Efavirenz ( EFV ), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS.
Common side effects include rash, nausea, headache, feeling tired, and trouble sleeping.
Efavirenz was approved for medical use in the United States in 1998.
Contents
1 Medical uses
1.1 Pregnancy and breastfeeding
2 Contraindications
3 Adverse effects
4 Drug interactions
5 Mechanism of action
5.1 Anti-HIV effects
5.2 Neuropsychiatric effects
6 Chemical properties
7 History
8 Society and culture
8.1 Pricing information
8.2 Recreational use
8.3 Brands
9 References
Medical uses
For HIV infection that has not previously been treated, the United States Department of Health and Human Services Panel on Antiretroviral Guidelines recommends the use of efavirenz in combination with tenofovir/emtricitabine (Truvada) as one of the preferred NNRTI-based regimens in adults and adolescents
Efavirenz is also used in combination with other antiretroviral agents as part of an expanded post-exposure prophylaxis regimen to reduce the risk of HIV infection in people exposed to a significant risk (e.g. needlestick injuries, certain types of unprotected sex, etc.).
Pregnancy and breastfeeding
Efavirenz is safe to use during the first trimester of pregnancy.
Contraindications
People who have taken this medication before and experienced an allergic reaction should avoid taking further efavirenz dosages. Hypersensitivity reactions include Steven-Johnson syndrome, toxic skin eruptions, and erythema multiforme.
Adverse effects
Neuropsychiatric effects are the most common adverse effects, and include disturbed sleep (including nightmares, insomnia, disrupted sleep, and daytime fatigue), dizziness, headaches, vertigo, blurred vision, anxiety, and cognitive impairment (including fatigue, confusion, and memory and concentration problems), and depression, including suicidal thinking.
Rash and nausea may occur.
Use of efavirenz can produce a false positive result in some urine tests for marijuana.
Efavirenz may lengthen the QT interval so should not be used in people with or at risk of torsades de pointes.
Efavirenz may cause convulsions in adult and pediatric populations who have a history of seizures.
Drug interactions
Efavirenz is broken down in the liver by enzymes that belong to the cytochrome P450 system, which include both CYP2B6 and CYP3A4. People who are taking both efavirenz and other drugs metabolized by the same enzymes might need the dose of their drugs to be increased or decreased.
One group of drugs that efavirenz affects is protease inhibitors, which are used for HIV/AIDS. Efavirenz will lower the blood levels of most protease inhibitors, including aprenavir, atazanavir, and indinavir. At lowered levels, protease inhibitors may not be effective in people taking both drugs, which means the virus that causes HIV/AIDS won’t be stopped from replicating and may become resistant to the protease inhibitor.
Efavirenz also affects antifungal drugs, which are used for fungal infections such as urinary tract infections. Similar to the effect seen with protease inhibitors, efavirenz lowers the blood levels of antifungal drugs like voriconazole, itraconazole, ketoconazole, and posaconazole. As a result of lowered levels, antifungal drugs may not be effective in people taking both drugs, which means that the fungi that cause the infection may become resistant to the antifungal.
Mechanism of action
Anti-HIV effects
Efavirenz falls in the NNRTI class of antiretrovirals. Both nucleoside and non-nucleoside RTIs inhibit the same target, the reverse transcriptase enzyme, an essential viral enzyme which transcribes viral RNA into DNA. Unlike nucleoside RTIs, which bind at the enzyme’s active site, NNRTIs act allosterically by binding to a distinct site away from the active site known as the NNRTI pocket.
Efavirenz is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class.
As most NNRTIs bind within the same pocket, viral strains which are resistant to efavirenz are usually also resistant to the other NNRTIs, nevirapine and delavirdine. The most common mutation observed after efavirenz treatment is K103N, which is also observed with other NNRTIs.
Neuropsychiatric effects
As of 2016 the mechanism of efavirenz’ neuropsychiatric adverse effects was not clear.
Chemical properties
Efavirenz is chemically described as ( S )-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2 H -3,1-benzoxazin-2-one. Its empirical formula is C 14 H 9 ClF 3 NO 2. Efavirenz is a white to slightly pink crystalline powder with a molecular mass of 315.68 g/mol. It is practically insoluble in water (<10 µg/mL). History Efavirenz was approved by the FDA on September 21, 1998, making it the 14th approved antiretroviral drug. On February 17, 2016, the FDA approved the generic tablet formulation to be produced by Mylan. In late-2018, Thailand's Government Pharmaceutical Organization (GPO) announced that it will produce efavirenz after receiving WHO approval. Efavirenz code name is DMP 266, discovered by Du pont Pharma. European countries are set to receive the license for manufacturing of Efavirenz in May 1999. Society and culture Pricing information A one-month supply of 600 mg tablets costs approximately US$1,010 in July 2016. In Thailand, a one month supply of efavirenz + Truvada, as of June 2012, cost 2,900 baht ( US$90 ), and there is a social program for patients who cannot afford the medication. As of 2018 In South Africa, a license has been granted to generics giant Aspen Pharmacare to manufacture, and distribute to Sub-Saharan Africa, a cost-effective antiretroviral drug. Recreational use Abuse of efavirenz by crushing and smoking the tablets for supposed hallucinogenic and dissociative effects has been reported in South Africa, where it is used in a mixture known as whoonga and nyaope. Brands As of 2016, efavirenz was marketed in various jurisdictions under the brand names Adiva, Avifanz, Efamat, Efatec, Efavir, Efavirenz, Efcure, Eferven, Efrin, Erige, Estiva, Evirenz, Filginase, Stocrin, Sulfina V, Sustiva, Virorrever, and Zuletel. As of 2016, the combination of efavirenz, tenofovir, and emtricitabine was marketed in various jurisdictions under the brand names Atripla, Atroiza, Citenvir, Oditec, Teevir, Trustiva, Viraday, and Vonavir. As of 2016, the combination of efavirenz, tenofovir, and lamivudine was marketed under the brand name Eflaten.

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Additional information about the drug Nevirapine


Nevirapine ( NVP ), marketed under the trade name Viramune among others, is a medication used to treat and prevent HIV/AIDS, specifically HIV-1.
Common side effects include rash, headache, nausea, feeling tired, and liver problems.
Nevirapine was approved for medical use in the United States in 1996.
Contents
1 Medical uses
1.1 Preventing mother-to-child transmission
2 Adverse effects
3 Drug interactions
4 Mechanism of action
5 History
6 Society and culture
7 References
Medical uses
Nevirapine is used in adults and in children 6 years of age infected with HIV-1 as part of combination antiretroviral treatment (ART or cART). Mono treatment use of nevirapine is not indicated due to increased risk of resistance.
Nevirapine in triple combination therapy has been shown to suppress viral load effectively when used as initial antiretroviral therapy ( i.e., in antiretroviral-naive patients).
This drug is generally only to be considered for used in HIV-1 infected population once CD4 cell counts are very low.
Although concerns have been raised about nevirapine-based regimens in those starting therapy with high viral load or low CD4 count, some analyses suggest that nevirapine may be effective in this group of people.
Nevirapine may also form a useful component of salvage regimens after virological failure, usually in combination with one or more PIs as well as nucleotide reverse transcriptase inhibitor (NRTIs), especially in those who have not previously taken an NNRTI.
Dosing in children is based on body surface area (BSA),
Preventing mother-to-child transmission
A single dose of nevirapine given to both mother and child reduced the rate of HIV transmission by almost 50% compared with a very short course of zidovudine (AZT) prophylaxis, in a clinical trial in Uganda.
A major concern with this approach is that NNRTI resistance mutations are commonly observed in both mothers and infants after single-dose nevirapine,
Adverse effects
The most common adverse effect of nevirapine is the development of mild or moderate rash (13%).
Nevirapine may cause severe or life-threatening liver toxicity, usually emerging in the first six weeks of treatment.
Cases of immune reconstitution syndrome and fat redistribution have also been observed with this drug.
U.S. Food and Drug Administration recommends stopping nevirapine if a person experiencing:
sign and symptoms of liver issues such as hepatitis
increased transaminases in addition to rash or systemic symptoms
formation of rash with systemic symptoms
severe skin or hypersensitivity reactions
Additionally, U.S. FDA recommends monitoring closely for first 6 weeks of therapy for above symptoms as there is high risk during this time. Monitor for up to the first 18 weeks of treatment and if a patient experiences 1) hepatitis plus rash or other systemic symptoms or 2) severe hypersensitivity or skin rash, nervirapine should not be restarted.
Drug interactions
Nevirapine is a substrate for liver CYP3A and CYP2B6 enzymes. Concomitant administration of drugs that are inhibitors of these enzymes may increase serum nevirapine levels significantly. Some examples of these drugs include ritonavir, fosamprenavir, and fluconazole. On the other hand, drugs that are inducers of these enzymes such as rifampicin may lower serum nevirapine levels.
In addition, concomitant use of St. John’s wort (Hypericum perforatum) or St. John’s wort containing products may significantly lower nevirapine levels.
Nevirapine is an inducer of cytochrome P450 isoenzymes CYP3A4 and CYP2B6. It may reduce levels of several co-administered drugs including the antiretrovirals efavirenz, indinavir, lopinavir, nelfinavir and saquinavir, as well as clarithromycin, ketoconazole, forms of hormonal contraception, and methadone.
Mechanism of action
Nevirapine shown in ball and stick structure.
Nevirapine falls in the non-nucleoside reverse transcriptase inhibitor (NNRTI) class of antiretrovirals.
Nevirapine is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class.
Resistance to nevirapine develops rapidly if viral replication is not completely suppressed. As all NNRTIs bind within the same pocket, viral strains which are resistant to nevirapine are usually also resistant to the other NNRTIs, efavirenz and delavirdine. However, second generation NNRTIs like rilpivirine and etravirine are effective in treatment for HIV strains resistant to nevirapine and other first generation drugs in that same class.
History
Nevirapine was discovered by Hargrave et al. at Boehringer Ingelheim Pharmaceuticals, Inc., one of the Boehringer Ingelheim group of companies. It is covered by U.S. Patent 5,366,972 and corresponding foreign patents. Nevirapine was the first NNRTI approved by the U.S. Food and Drug Administration (FDA). It was approved June 21, 1996 for adults and September 11, 1998 for children. It was also approved in Europe in 1997.
Society and culture
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Additional information about the drug Amoxapine


Amoxapine, sold under the brand name Asendin among others, is a tricyclic antidepressant (TCA). It is the N- demethylated metabolite of loxapine. Amoxapine first received marketing approval in the United States in 1992 (approximately 30 to 40 years after most of the other TCAs were introduced in the United States).
Contents
1 Medical uses
2 Contraindications
2.1 Lactation
3 Side effects
4 Overdose
5 Pharmacology
5.1 Pharmacodynamics
5.2 Pharmacokinetics
6 Society and culture
6.1 Brand names
7 See also
8 References
Medical uses
Amoxapine is used in the treatment of major depressive disorder. Compared to other antidepressants it is believed to have a faster onset of action, with therapeutic effects seen within four to seven days.
Contraindications
As with all FDA -approved antidepressants it carries a black-box warning about the potential of an increase in suicidal thoughts or behaviour in children, adolescents and young adults under the age of 25.
Severe cardiovascular disorders (potential of cardiotoxic adverse effects such as QT interval prolongation)
Uncorrected narrow angle glaucoma
Acute recovery post- myocardial infarction
Its use is also advised against in individuals concurrently on monoamine oxidase inhibitors or if they have been on one in the past 14 days and in individuals on drugs that are known to prolong the QT interval (e.g. ondansetron, citalopram, pimozide, sertindole, ziprasidone, haloperidol, chlorpromazine, thioridazine, etc.).
Lactation
Its use in breastfeeding mothers not recommended as it is excreted in breast milk and the concentration found in breast milk is approximately a quarter that of the maternal serum level.
Side effects
Adverse effects by incidence:
Note: Serious (that is, those that can either result in permanent injury or are irreversible or are potentially life-threatening) are written in bold text.
Very common (>10% incidence) adverse effects include:
Constipation
Dry mouth
Sedation
Common (1–10% incidence) adverse effects include:
Anxiety
Ataxia
Blurred vision
Confusion
Dizziness
Headache
Fatigue
Nausea
Nervousness/restlessness
Excessive appetite
Rash
Increased perspiration (sweating)
Tremor
Palpitations
Nightmares
Excitement
Weakness
ECG changes
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Human
H 4
6,310
Human
mACh
1,000
Human
Values are K i (nM). The smaller the value, the more strongly the drug binds to the site.
Amoxapine possesses a wide array of pharmacological effects. It is a moderate and strong reuptake inhibitor of serotonin and norepinephrine, respectively,
7-Hydroxyamoxapine, a major active metabolite of amoxapine, is a more potent dopamine receptor antagonist and contributes to its neuroleptic efficacy,
Pharmacokinetics
Amoxapine is metabolised into two main active metabolites: 7-hydroxyamoxapine and 8-hydroxyamoxapine.
Amoxapine
7-hydroxyamoxapine
8-hydroxyamoxapine
Compound
t 1/2 (hr)
t max (hr)
C SS (ng/mL)
Protein binding
V d
Excretion
Amoxapine
8
1-2
17-93 ng/mL (divided dosing), 13-209 ng/mL (single daily dosing)
90%
0.9-1.2 L/kg
Urine (60%), feces (18%)
8-hydroxyamoxapine
30
5.3 (single dosing)
158-512 ng/mL (divided dosing), 143-593 ng/mL (single dose)
?
?
?
7-hydroxyamoxapine
6.5
2.6-5.4 (single dosing)
?
?
?
?
Where:
– t 1/2 is the elimination half life of the compound.
– t max is the time to peak plasma levels after oral administration of amoxapine.
– C SS is the steady state plasma concentration.
– protein binding is the extent of plasma protein binding.
– V d is the volume of distribution of the compound.
Society and culture
Brand names
Brand names for amoxapine include (where † denotes discontinued brands):
Adisen ( KR )
Amolife ( IN )
Amoxan ( JP )
Asendin† (previously marketed in CA, NZ, US )
Asendis† (previously marketed in IE, UK )
Défanyl ( FR )
Demolox ( DK †, IN, ES †)
Oxamine ( IN )
Oxcap ( IN )
See also
Loxapine

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