Pharmacology

  

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This article is intended to provide a broad overview of pharmacology and medications often used in either community or institutional pharmacy settings and is not intended as sole means towards determining diagnosis and/or treatment of an individual.

This article will cover the following knowledge areas:

  • Generic and brand names of pharmaceuticals
  • Therapeutic equivalence
  • Drug interactions (e.g., drug-disease, drug-drug, drug-dietary supplement, drug-OTC, drug-laboratory, drug-nutrient)
  • Strengths/dose, dosage forms, physical appearance, routes of administration, and duration of drug therapy
  • Common and severe side or adverse effects, allergies, and therapeutic contraindications associated with medications
  • Dosage and indication of legend, OTC medications, herbal and dietary supplements

Contents

Terminology

To get started in this chapter, there are some terms that should be defined.

pharmacology - The term pharmacology is derived from to Greek words "pharmakon" and "logos". Pharmakon can mean sacrament, remedy, poison, talisman, cosmetic, perfume or intoxicant, but in this case it can be broadly defined as drug. Logos can be translated as a principle of order and knowledge. By combining the terms you can see that pharmacology is concerned with the knowledge of drugs.

OTC - Over the counter medications are drugs that do not require the use of a prescription for a patient to obtain it. These medications are generally considered sufficiently safe for a patient to acquire and self medicate with by following the instructions included on the vial.

legend - Legend drugs are medications that require a prescription prior to dispensing. These medications may or may not be considered abusable, but consultation with a medical professional that has prescribing authority is necessary due to the complex health conditions that these medications may be able to treat or ameliorate. Often, you will see the phrase "Rx only" used to denote legend drugs.

controlled substances - Controlled substances are medications with restrictions due to abuse potential. There are 5 schedules of controlled substances with various prescribing guidelines based on abuse potential counter balanced by potential medicinal benefit as determined by the Drug Enforcement Administration and individual state legislative branches.

brand name - This is the manufacturers trademark designation. Each brand name is owned by the company and begins with a capital letter, and it is protected by a trademark. Drugs often have several brand names. The terms trade name and proprietary name may also be used interchangeably with brand name.

generic name - This is the official non-proprietary name assigned by the manufacturer with the approval of the USAN (United States Adopted Name) Council. The Federal Food and Drug Administration (FDA) requires that each drug has a generic name even if currently it is only available as a brand name product. A generic name may also be referred to as the non-proprietary name.

therapeutic equivalents - Drug products are considered to be therapeutic equivalents only if they are available in the same dosage strength, dosage form, achieve the same blood levels, and if they can be expected to have the same clinical effect and safety profile when compared to the original innovator drug. To ensure that a specific generic product is considered to be a therapeutic equivalent, it is recommended that you refer to the Orange Book, a publication from the Food and Drug Administration (FDA). If the the products being compared in the Orange Book are considered therapeutic equivalents, it will be given a Therapeutic Equivalence (TE) Code of "A". If the products are not considered therapeutic equivalents, they will be given a TE Code of "B". Sometimes these will be referred to as "A" ratings and "B" ratings.

classification - This is how a medication is grouped and is typically defined according to its use in treating a particular disease or disorder. A potential source of confusion is that many medications could be grouped multiple ways. An example of this it aspirin can be classified as an analgesic, antipyretic, and anti-inflammatory agent.

indication - This is the primary condition(s) treated by a particular drug. This may include both FDA approved uses as well as off-label (generally based on scientific studies but lacking FDA approval) medication uses.

dosage form - A dosage form is the physical form of a dose of medication, such as capsule, patch, or injection. The route of administration is dependent on the dosage form of a given drug. As an example, persistent vomiting may make it difficult to use an oral dosage form, therefore an antiemetic in suppository form may be desirable.

interactions - Medications have the potential to interact with other medications, dietary supplements, and constituents of various foods. Medications may also interact with various diseases.

Common medications

Pharmacy technicians should be able to categorize drugs into major therapeutic classifications and be able to briefly describe the therapeutic use of each drug. Technicians should also be able to correlate brand name medications with the generic names.

The following subsections will break the drugs down into various therapeutic classes with descriptions of these classes followed by a list of generic drug names accompanied by their most common brand names and commercially available dosage forms. These lists are not to be considered comprehensive, but instead just provide some of the more common items to serve as a quick refresher. If you want more information on a particular drug, an excellent free (registration required) resource is Medscape at http://reference.medscape.com.

Anti-infective agents

An anti-infective (also called an antimicrobial) is a substance that kills or inhibits the growth of microbes such as bacteria, fungi, protozoans or viruses. In this section we will look at antibiotics, antifungals, amebicides, and antivirals.

Bacteria treated by antibiotics are usually broken into two categories, gram positive and gram negative.

Gram-positive bacteria are those that are stained dark blue or violet by Gram staining. This is in contrast to Gram-negative bacteria, which cannot retain the crystal violet stain, instead taking up the counterstain (safranin or fuchsin) and appearing red or pink. Gram-positive organisms are able to retain the crystal violet stain because of the high amount of peptidoglycan in the cell wall. Gram-positive cell walls typically lack the outer membrane found in Gram-negative bacteria.

Penicillin Derivatives

Penicillin derivatives act by preventing cell wall synthesis during active replication and are therefore bactericidal. Penicillin derivatives have a chemical structure referred to as a beta-lactam ring which is what allows it to attach to the bacteria. Penicillins are used in the treatment of bacterial infections caused by susceptible, usually Gram-positive, organisms. The most common side effects are allergic reactions including rash, hives, or anaphylactic shock.

amoxicillin (Amoxil, Moxatag, Trimox) - oral solution, capsule, tablet, chewable tablet, extended-release tablet
ampicillin (Principen) - capsules, oral suspension, powder for injection
nafcillin (Nafcil) - injectable solution, powder for injection
oxacillin (Bactocill) - infusion solution, oral solution, powder for injection
penicillin G (Bicillin, Wycillin) - premixed injectable solution, powder for injectable solution
penicillin V potassium (Pen Vee K, Veetids) - oral solution, tablet
piperacillin (Pipracil) - powder for injection
ticarcillin (Ticar) - powder for injection

Penicillin Derivatives with Beta-Lactamase Inhibitors

Sometimes bacteria become resistant to penicillin, and one such mechanism of action for them to do that is by creating beta-lactamase which breaks down the beta-lactam ring in penicillins preventing them from attaching to the bacteria walls. There is a chemical class that can prevent this called beta-lactamase inhibitors that are often coupled with penicillins.

amoxicillin & clavulanate (Augmentin) - oral suspension, tablet, chewable tablet
ampicillin & sulbactam (Unasyn) - injectable solution, powder for solution
piperacillin & tazobactam (Zosyn) - powder for injection
ticarcillin & clavulanate (Timentin) - powder for injection, infusion solution

Carbapenems

Carbapenems are a class of beta-lactam antibiotics with a broad spectrum of antibacterial activity, and have a structure which renders them highly resistant to beta-lactamases.

ertapenem (Invanz) - powder for injection
imipenem & cilastin (Primaxin) - powder for injection
meropenem (Merrem) - powder for injectable solution

Cephalosporins

The cephalosporins are bactericidal antibiotics that have chemical structures similar to those of penicillins and therefor have the same mechanism of action. Also, due to their similar chemical structure to penicillin, there is a 7-10% potential of cross sensitivity. The cephalosporins are considered to be broad spectrum drugs. Their two main uses are as substitutes for penicillins in cases of allergy or bacterial resistance and in the treatment of certain gram negative infections.

cefaclor (Ceclor) - capsule, tablet extended-release
cefazolin (Kefzol) - powder for injection
cefdinir (Omnicef) - capsule, oral suspension
cefepime (Maxipime) - infusion solution, powder for injection
cefotaxime (Claforan) - injectable solution, powder for injection
cefotetan (Cefotan) - injectable solution, powder for injection
ceftaroline (Teflaro) - powder for injection
ceftazidime (Fortaz) - injectable solution, powder for injection
ceftriaxone (Rocephin) - injectable solution, powder for injection
cephalexin (Keflex) - capsule, film-coated tablet, oral suspension, tablet for oral suspension

Aminoglycosides

The aminoglycosides are a group of bactericidal antibiotics whose antibacterial spectrum mainly includes gram-negative bacilli. Aminoglycosides have poor oral absorption, therefore if systemic effects are desired they are usually given IV or IM. Aminoglycosides are both nephrotoxic (kidney) and ototoxic (ear).

amikacin (Amikin) - injectable solution
gentamicin (Garamycin) - injectable solution, ophthalmic ointment, ophthalmic suspension
kanamycin (Kantrex) - injectable solution
tobramycin (Nebcin, Tobi, Tobrex) - injectable solution, nebulizer solution, ophthalmic ointment, ophthalmic solution
tobramycin & dexamethasone (TobraDex) - ophthalmic ointment, ophthalmic suspension - This is a combination of an aminoglycoside and a corticosteroid.

Tetracyclines

The tetracyclines (a group of broad-spectrum bacteriostatic antibiotics) are clinically useful in both gram-positive and gram-negative infections.

When ingested, it is usually recommended that tetracyclines should be taken with a full glass of water, either two hours after eating or one hour before eating. This is partly because tetracycline binds easily with magnesium, aluminum, iron, and calcium, which reduces its ability to be completely absorbed by the body. Dairy products or preparations containing iron are not recommended directly after taking the drug.

Side effects from tetracyclines are not always common, but of particular note is possible photosensitive allergic reaction which increases the risk of sunburn under exposure to UV light from the sun or other sources. Tetracyclines are teratogens due to the likelihood of causing teeth discoloration in the fetus as they develop in infancy. For this same reason, tetracyclines are contraindicated for use in children under 12 years of age.

doxycycline (Vibramycin) - capsule, powder for injection, syrup, tablet, delayed-release tablet
minocycline (Minocin) - oral suspension, tablet, capsule, extended-release tablet, intravenous injection
tetracycline (Sumycin) - capsule, tablet
tigecycline (Tygacil) - powder for injection

Sulfonamides

Sulfonamides are a group of synthetic bacteriostatic drugs which are effective against both gram-positive and gram-negative infections. Approximately 3% of people using sulfonamides report side effects, the most common of which are hypersensitivity reactions such as rash and hives, but some patients may have more severe reactions.

Sulfonamides have the potential to crystallize in the kidneys, due to their low solubility. This is a very painful experience, so patients are recommended to take these medication with large amounts of water.

silver sulfidiazine (Silvadene) - cream
sulfamethoxazole & trimethoprim, SMZ & TMP (Bactrim, Septra, Co-Trimoxazole) - injected solution, oral solution, tablet
sulfasalazine (Azulfidine) - tablet, extended-release tablet

Macrolide Antibiotics

The term macrolide refers to the large chemical ring structure that is characteristic of these antibiotics. These antibiotics inhibit bacterial protein synthesis and can be bacteriostatic or bactericidal. Food effects oral absorption of these drugs, although they frequently cause GI problems which may warrant taking them with food. Macrolides may interfere with some medications that require liver biotransformation such as digoxin, warfarin, and cyclosporine therefore a different antibiotic choice may be desirable if a patient is currently using any of those medications.

azithromycin (Zithromax, AzaSite) - oral suspension, powder for injection, powder for oral suspension, extended-release powder for oral suspension, tablet, ophthalmic solution
clarithromycin (Biaxin) - oral suspension, tablet, extended-release tablet
erythromycin (Erythrocin, E-Mycin) - tablet, delayed-release tablet, dispertab, injection, oral suspension, ophthalmic ointment

Fluoroquinolones

The fluoroquinolones, often just called quinolone antibiotics, are synthetic antimicrobial agents that are a broad spectrum bactericidal, especially against gram-negative organisms. A black box warning has been added to all fluoroquinolones involving an increased risk of developing tendinitis and tendon rupture in patients of all ages taking fluoroquinolones for systemic use. This risk is further increased in individuals over 60 years of age, taking corticosteroid drugs, and have received kidney, heart, or lung transplants.

ciprofloxacin (Cipro) - infusion solution, oral suspension, tablet, extended-release tablet, ophthalmic solution, ophthalmic ointment, otic solution
levofloxacin (Levaquin) - injectable solution, premix infusion solution, oral solution, tablet, ophthalmic solution
moxifloxacin (Avelox) - injectable solution, tablet, opthalmic solution
ofloxacin (Floxin) - tablet, ophthalmic solution, otic solution

Miscellaneous Antibiotics

Some common antibiotics are the only drugs in their respective classes. The following listed medications are examples of those. These drugs each have their own side effects and precautions, for example, IV use of vancomycin may cause a reaction known as red man syndrome characterized by flushing and/or rash that affects the face, neck, and upper torso.

aztreonam (Azactam) - infusion solution, powder for injection
clindamycin (Cleocin) - capsule, injectable solution, oral solution, vaginal cream, vaginal suppository
daptomycin (Cubicin) - injectable solution
linezolid (Zyvox) - injectable solution, oral suspension, tablet
mupirocin (Bactroban) - cream, topical ointment, nasal ointment
nitrofurantoin (Macrobid) - capsule, oral suspension
vancomycin (Vancocin) - capsule, injectable solution, powder for injection

Antifungals

An antifungal drug is medication used to treat fungal infections such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others.

Antifungals work by exploiting differences between mammalian and fungal cells to kill off the fungal organism without dangerous effects on the host. Unlike bacteria, both fungi and humans are eukaryotes. Thus fungal and human cells are similar at the molecular level. This means it is more difficult to find a target for an antifungal drug to attack that does not also exist in the infected organism. Consequently, there are often side-effects to some of these drugs. Many of these agents are hepatotoxic (liver) and liver function and enzymes must be monitored. It is not uncommon for therapy to last for several months.

amphotericin B (Fungizone) - powder for injection, injectable lipid complex, cream, lotion, ointment
betamethasone & clotrimazole (Lotrisone) - cream, lotion - This is a combination of a corticosteroid and an antifungal.
clotrimazole (Gyne-Lotrimin, Mycelex) - troche, vaginal cream, vaginal tablet, cream, topical solution, lotion, powder
fluconazole (Diflucan) - injected solution, oral suspension, tablet nystatin (Mycostatin, Nilstat) - oral powder, oral suspension, oral tablet, troche, cream, ointment, powder, vaginal tablet
terbinafine (Lamisil) - tablet, oral granules, cream, topical solution

Amebicides

An amebicide (or amoebicide) is an agent used in the treatment of amoebic infections. Alcohol use should be avoided while taking metronidazole because concurrent use may cause nausea, vomiting, flushing of the skin, tachycardia, and shortness of breath.

metronidazole (Flagyl) - capsule, tablet, extended-release tablet, infusion solution, topical gel, topical cream, topical lotion, vaginal gel
pentamidine (Pentam) - powder for injection, powder for nebulizer solution

Antimalarial Drugs

Antimalarial drugs are agents used to prevent and cure malaria. Some antimalarial drugs, such as hydroxychloroquine, are also used to treat conditions like rheumatoid arthritis and lupus. One of the most serious side effects is a toxicity in the eye (this primarily occurs with chronic use).

hydroxychloroquine (Plaquenil) - tablet
quinine sulfate (Qualaquin) - capsule

Antivirals

Antiviral drugs are a class of medication used specifically for treating viral infections. Like antibiotics, specific antivirals are used for specific viruses. They are relatively harmless to the host, and therefore can be used to treat infections. They should be distinguished from viricides, which actively deactivate virus particles outside the body.

Most of the antivirals now available are designed to help deal with HIV; herpes viruses, best known for causing cold sores and genital herpes, but actually causing a wide range of diseases; the hepatitis B and C viruses, which can cause liver cancer; and influenza A and B viruses. Researchers are now working to extend the range of antivirals to other families of pathogens.

Antiviral drugs work by inhibiting the virus ether before it enters the cell, stopping it from reproducing, or in some cases preventing it from exiting the cell. However, like antibiotics, viruses may evolve to resist the antiviral drug.

acyclovir (Zovirax) - injectable solution, oral suspension, powder for injection, tablet, capsule, topical cream, topical ointment
ganciclovir (Cytovene) - capsule, powder for injection, oral solution, implant, ophthalmic gel
valacyclovir (Valtrex) - tablet

Glucocorticosteroids

Glucocorticosteriods (glucocorticoids) are steroids used to treat inflammation and various allergic conditions. They are similar to the steroid created in the adrenal cortex although they could be either from natural sources or synthetically manufactured. As your body naturally produces a glucocorticoid, introducing an exogenous source through medication interferes with your bodies negative feedback loop for production of these steroids. This is why it is often necessary to taper a patient off of a steroid so their body slowly start creating its own endogenous source of steroids again.

Long term use of glucocorticoids can have the following negative effects: thinning of skin, decrease wound healing, stunting pediatric growth, moon-face, obesity, and diabetes mellitus.

Short-Acting Steroids

hydrocortisone (Cortef) - tablet, oral suspension, powder for injection, rectal cream, enema, foam, suppositories, topical cream, lotion, gel, topical solution, ointment, pledget

Intermediate-Acting Steroids

fluticasone (Flovent HFA, Flonase) - aerosol inhaler, disk inhaler, nasal spray, cream, ointment, lotion
methylprednisolone (Depo-Medrol, Medrol, Solu-Medrol) - tablet, injectable suspension, powder for injection
prednisolone (Delta-Cortef) - oral solution, tablet, ophthalmic suspension, ophthalmic solution
prednisone (Deltasone) - oral solution, tablet
triamcinolone, TAC (Azmacort, Nasocort AQ, Kenalog) - nasal spray, inhalation aerosol, intravitreal injection, cream, ointment, paste, topical spray

Long-Acting Steroids

dexamethasone (Decadron) - tablet, injectable suspension, elixir, oral solution, oral concentrate, ointment, ophthalmic solution, ophthalmic suspension, intravitreal implant

Drugs affecting the sympathetic nervous system

The sympathetic nervous system is part of the autonomic nervous system that tends to act in opposition to the parasympathetic nervous system, by speeding up the heartbeat and causing contraction of the blood vessels. It regulates the function of the sweat glands and stimulates the secretion of glucose in the liver. The sympathetic nervous system is usually activated under conditions of stress cause the 'fight or flight' response.

The sympathetic nervous system can be excited or inhibited through either stimulating or inhibiting adrenergic receptors. These adrenergic receptors are normally stimulated by endogenous norepinephrine, but they can be stimulated by exogenous chemicals of either natural or synthetic origin. These adrenergic receptors can be further broken up into subgroups called alpha-1, alpha-2, beta-1, and beta-2 adrenergic receptors. Excitation of alpha-1 and alpha-2 adrenergic receptors causes contraction of smooth muscle resulting in vasoconstriction of most blood vessels, contraction of sphincter muscles in the GI and urinary tract, and dilation of the pupil of the eye (mydriasis). Stimulation of beta-1 adrenergic receptors cause stimulation of the heart (increased heart rate and force of contraction). Stimulation of beta-2 adrenergic receptors cause bronchodilation. Inhibition (blocking) of these receptors cause the opposite effect to occur.

Let's look at drugs that affect these various receptors.

Adrenergic Agonists

These drugs stimulate all the adrenergic receptors to varying degrees and will therefore have the effects related to stimulation of these receptors. This allows these drugs to be used for a multitude of purposes such as acute hypotension (ephedrine, NE, PE), cardiac arrest (EPI, NE), severe asthma (EPI), bronchodilation (ephedrine), anaphylaxis (EPI), congestion (PE), and can be used to dilate pupils (PE).

ephedrine - injectable solution
epinephrine, EPI (EpiPen, Racepinephrine) - autoinjector, injectable solution, solution for nebulization
norepinephrine, NE (Levophed) - injectable solution
pseudoephedrine, PE (Sudafed) - tablet, syrup

Alpha-2 Adrenergic Agonists

Alpha-2 agonists, despite stimulating the alpha-2 adrenergic receptors actually function against the sympathetic nervous system and sometimes will be classified as sympathetic blocking (sympatholytic) drugs. The net result is a decrease in cardiac output and vasodilation making them useful in the treatment of hypertension.

clonidine (Catapres, Catapres TTS) - injectable solution, extended-release oral suspension, patch, tablet, extended-release tablet
guanfacine (Tenex) - tablet

Alpha-Adrenergic Blocking Agents

Alpha-adrenergic blocking drugs are primarily used to treat benign prostatic hypertrophy (BPH). These medications also cause vasodilation and reduced blood pressure, making them suitable choices for treating hypertension.

doxazosin (Cardura, Cardura XL) - tablet, extended-release tablet
tamsulosin (Flomax) - capsule
terazosin (Hytrin) - capsule

Beta-Adrenergic Blocking Agents

By blocking the beta-adrenergic receptors you can decrease the heart rate and the force of contractions causing a decrease in blood pressure. This means the drugs can treat hypertension, angina pectoris, tachycardia, and arrhythmias.

atenolol (Tenormin) - Tablet
bisoprolol (Zebeta) - Tablet
carvedilol (Coreg, Coreg CR) - extended-release capsule, tablet
labetalol (Trandate) - injectable solution, tablet
metoprolol (Lopressor, Toprol XL) - injectable solution, tablet, extended-release tablet
nebivolol (Bystolic) - tablet
propranolol (Inderal, Inderal LA) - oral solution, injectable solution, tablet, extended-release capsule
timolol (Timol, Timoptic, Timoptic XE) - ophthalmic solution, gel forming ophthalmic solution

Drugs affecting the parasympathetic nervous system

The parasympathetic nervous system is part of the autonomic nervous system that tends to act in opposition to the sympathetic nervous system, by primarily regulating body functions during rest, digestion, and waste regulation. Stimulation of the parasympathetic system increases the activity of the gastrointestinal and genitourinary system while decreasing the activity of the cardiovascular system.

Cholinergic Drugs

The parasympathetic system is regulated by cholinergic receptors. The naturally occurring chemical that stimulates these receptors is called acetylcholine (ACH). Drugs that mimic ACH are therefor called cholinergic drugs. The conditions treated by this class of drugs varies widely. Donepezil and galantamine are each primarily used to treat Alzheimer's disease, while neostigmine is used to treat myasthenia gravis, and is an antidote for nondepolarizing neuromuscular blocking drugs (a group of drugs often used to create a neuromuscular blockade during surgery).

donepezil (Aricept, Aricept ODT) - tablet, orally disintegrating tablet
galantamine (Reminyl) - tablet, extended-release tablet, oral solution
neostigmine (Prostigmin) - injectable solution, tablet

Anticholinergic Drugs

A naturally occurring chemical that works opposite of ACH is acetylcholinesterase, and therefor drugs that mimic acetylcholinesterase are often referred to as anticholinergic drugs. The conditions treated by this group of drugs also varies widely. Atropine can be used to increase the heart rate, anesthesia premedication, reversal of cholinergic drugs, treatment of GI spasticity, mydriasis, and enuresis treatment. Dicyclomine is typically used to treat GI disorders such as ulcers and colitis. Oxybutynin and tolterodine are typically used in the treatment of overactive bladder.

atropine (AtroPen, IsoptoAtropine) - injectable solution, tablet, ophthalmic solution, ophthalmic ointment
dicyclomine (Bentyl) - capsule, injectable solution, syrup, tablet
oxybutynin (Ditropan, Ditropan XL) - tablet, controlled-release tablet, syrup, transdermal patch, gel
tolterodine (Detrol, Detrol LA) -tablet, extended-release capsule

Skeletal muscle relaxants

Skeletal muscle relaxants are used to treat conditions such as muscle spasticity and to relax muscle tone during surgeries. Medication that block muscle contraction within the spinal cord are referred to as centrally acting skeletal muscle relaxants, conversely peripherally acting skeletal muscle relaxants inhibit muscle contraction at the neuromuscular junction (NMJ).

All patients using skeletal muscle relaxants should avoid additional items that will depress the CNS or impair neuromuscular function such as alcohol, sedatives, and tranquilizers. There is also concern over abuse of these drugs, whether on their own or being used with other medications. Hence, carisoprodol was recently made a schedule IV controlled substance.

Peripherally Acting Skeletal Muscle Relaxants

Peripherally acting skeletal muscle relaxants are primarily used to prevent muscle contractions during surgeries or procedures where reflexes need to be suppressed (i.e., intubation). They can further be broken into two major subgroups depolarizing (succinylcholine) and nondepolarizing (cisatracurium, pancuronium, rocuronium, and vecuronium).

cisatracurium (Nimbex) - injectable solution
pancuronium (Pavulon) - injectable solution
rocuronium (Zemuron) - injectable solution
succinylcholine, SUX (Anectine) - injectable solution
vecuronium (Norcuron) - powder for injection

Centrally Acting Skeletal Muscle Relaxants

Centrally acting skeletal muscle relaxants are primarily used to treat muscle spasms that may be caused by overexertion, trauma, or nervous tension. Baclofen and tizanidine are also used to treat multiple sclerosis.

baclofen (Lioresal) - tablet, injectable solution
carisoprodol (Soma) CIV - tablet
cyclobenzaprine (Flexeril) - tablet, extended-release capsule
metaxalone (Skelaxin) - tablet
methocarbamol (Robaxin) - tablet, injectable solution
tizanidine (Zanaflex) - tablet, capsule

Local Anesthetics

Local anesthetics, as their name implies, causes a temporary loss of feeling in a confined area of the body. Local anesthetics can be broken into two major groups, amide local anesthetics and ester local anesthetics. Cocaine is also used as a local anesthetic because despite its abuse potential, it is the only local anesthetic that causes vasoconstriction.

Ester Local Anesthetics

In general ester local anesthetics have a short or moderate duration of action.

benzocaine (Solarcaine) - gel, topical solution, otic solution
cocaine CII - topical solution
tetracaine (Pontocaine) - injectable solution, powder for injection, throat spray, ophthalmic solution

Amide Local Anesthetics

Typically, amide local anesthetics have a long duration of action.

bupivacaine (Marcaine, Sensorcaine) - injectable solution
lidocaine (Xylocaine, Lidoderm) - injectable solution, infusion solution, oral solution, topical ointment, topical solution, topical jelly, patch

Medications for treating psychological conditions

Antipsychotic Drugs

Antipsychotic drugs, referred to as neuroleptics, are used to suppress the symptoms of schizophrenia and other psychotic conditions. Antipsychotics are associated with a range of side effects. Approximately two-thirds of patients will discontinue use due in part to adverse effects. Side effects may include acute dystonias, akathisia, parkinsonism, tardive dyskinesia, tachycardia, hypotension, impotence, lethargy, seizures, intense dreams or nightmares, and hyperprolactinaemia. Side effects from antipsychotics can be managed by a number of different drugs. For example, anticholinergics are often used to alleviate the motor side effects of antipsychotics. Some of the side-effects will appear after the drug has been used only for a long time. When discontinuing therapy, patients must be tapered off of these drugs.

clozapine (Clozaril) - tablet, orally disintegrating tablet
haloperidol (Haldol) - tablet, oral concentrate, injectable solution, injectable solution-decanoate
olanzapine (Zyprexa, Zyprexa Zydis) - tablet, orally disintegrating tablet, short-acting IM injection, extended-release suspension IM injection
quetiapine (Seroquel, Seroquel XR) - tablet, extended-release tablet
risperidone (Risperdal, Risperdal Consta) - tablet, orally-disintegrating tablet, oral solution, powder for injection
ziprasidone (Geodon) - capsule, powder for injection

Hypnotics

Hypnotics are primarily used to induce and maintain sleep, usually to treat insomnia. There are three major categories of hypnotics benzodiazepines, barbiturates, and nonbarbiturates. Other medications and substances that cause CNS depression (such as alcohol) should be avoided.

Benzodiazepines

Benzodiazepines are commonly used as anxiolytics, sedatives, hypnotics, anticonvulsants, and skeletal muscle relaxants.

alprazolam (Xanax) CIV - tablet, extended-release tablet, orally-disintegrating tablet, oral solution
clonazepam (Klonopin) CIV - tablet
diazepam (Valium) CIV - tablet, oral solution, rectal solution, injectable solution, intramuscular device
lorazepam (Ativan) CIV - tablet, oral concentrate, injectable solution
temazepam (Restoril) CIV - tablet

Barbiturates

Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, as hypnotics, and as anticonvulsants. Barbiturates also have analgesic effects, however these effects are somewhat weak, preventing barbiturates from being used in surgery in the absence of other analgesics.

phenobarbital (Luminal) CIV - tablet, elixir, injectable solution

Nonbarbiturate Hypnotics

Barbiturates, while strictly considered hypnotics, have been largely replaced by the newer nonbarbiturates for treating insomnia since barbiturates are know to cause a 'hangover' effect.

eszopiclone (Lunesta) CIV - tablet
ramelteon (Rozerem) - tablet
zaleplon (Sonata) CIV - capsule
zolpidem (Ambien, Ambien CR) CIV - tablet, extended-release tablet, sublingual tablet, oral spray

Antidepressants

An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder.

Antidepressants carry a black box warning that in short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults.

Tricyclic Antidepressants

The tricyclic antidepressants are used primarily in the clinical treatment of mood disorders such as major depressive disorder, dysthymia, and treatment-resistant variants. They are also used in the treatment of a number of other medical disorders, including anxiety disorders such as generalized anxiety disorder, social phobia also known as social anxiety disorder, obsessive-compulsive disorder, and panic disorder, post-traumatic stress disorder, body dysmorphic disorder, eating disorders like anorexia nervosa and bulimia nervosa, certain personality disorders such as borderline personality disorder, attention-deficit hyperactivity disorder, as well as chronic pain, neuralgia or neuropathic pain, and fibromyalgia, headache, or migraine, smoking cessation, tourette syndrome, trichotillomania, irritable bowel syndrome, interstitial cystitis, nocturnal enuresis, narcolepsy, insomnia, pathological crying and/or laughing, chronic hiccups, ciguatera poisoning, and as an adjunct in schizophrenia.

amitriptyline (Elavil) - tablet
doxepin (Sinequan) - capsule, tablet, oral concentrate

Selective Serotonin Reuptake Inhibitors

Selective Serotonin Reuptake Inhibitors (SSRIs) are believed to work by decreasing the central nervous system's neuronal uptake of serotonin (5-HT). While these drugs can be used for a very broad range of things, you will typically see them used for treating moderate to major depression, generalized anxiety disorder, panic disorders, social anxiety, post-traumatic stress disorder, premenstrual dysphoric disorder, and prevention of migraine.

citalopram (Celexa) - tablet, oral solution
escitalopram (Lexapro) - tablet, oral solution
fluoxetine (Prozac) - tablet, capsule, delayed-release capsule, oral solution
fluvoxamine (Luvox) - tablet, extended-release capsule
paroxetine (Paxil) - tablet, extended-release tablet, oral suspension

Serotonin-Noerpinephrine Reuptake Inhibitors

Serotonin-norepinephrine reuptake inhibitors (SNRIs) prevent the uptake of neuronal serotonin and norepinephrine and are a less potent inhibitor of dopamine reuptake. The increase in these chemicals is believed to be related to their use in treating depression and anxiety. Duloxetine is also commonly used to treat chronic musculoskeletal pain, diabetic peripheral neuropathic pain, and fibromyalgia.

desvenlafaxine (Pristiq) - extended-release tablet
duloxetine (Cymbalta) - capsule
venlafaxine (Effexor, Effexor XR) - tablet, extended-release tablet, extended-release capsule

Miscellaneous Antidepressants

The medications in this category have varied mechanisms of action, but all function as antidepressants. Bupropion is also used for seasonal affective disorder, and smoking cessation. Mirtazapine is also used for post-traumatic stress disorder (PTSD). Trazadone is used for a number of things including aggressive behavior, alcohol withdrawal, insomnia, and prevention of migraine.

bupropion (Wellbutrin, Zyban) - tablet, sustained-release tablet, extended-release tablet
mirtazapine (Remeron, Remeron SolTab) - tablet, orally-disintegrating tablet
trazadone (Desyrel, Desyrel Dividose) - tablet, extended-release tablet

Antianxiety Agent, Nonbenzodiazepine

While many anxiolytic agents are related to benzodiazepines, one popular alternative is buspirone. It has a high affinity for 5HT1 receptors and a moderate affinity for dopamine D2 receptors. Buspirone is considered to have very little abuse potential; so unlike benzodiazepines, it is not a controlled substance.

buspirone (BusPar) - tablet

Partial Nicotinic Receptor Antagonist

Varenicline is used as a smoking cessation aid without actually using any form of nicotine. There is a heightened caution with this drug about suicidal ideation (suicidal thoughts).

varenicline (Chantix) - tablet

Amphetamines

Amphetamines are commonly used to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy. Their ability to improve focus/concentration and boost energy levels has made this class of drugs very desirable for abuse, therefore all amphetamines are considered schedule II controlled substances. Side effects may consist of severe weight loss, also dependence may develop during use of this drug. Amphetamines can also raise the heart rate to dangerous levels.

amphetamine & dextroamphetamine (Adderall, Adderall XR) CII - tablet, capsule, extended-release capsule
dexmethylphenidate (Focalin, Focalin XR) CII - tablet, extended-release capsule
lisdexamfetamine (Vyvanse) CII - capsule
methylphenidate (Ritalin, Concerta, Daytrana) CII - tablet, chewable tablet, extended-release tablet, capsule, extended-release capsule, oral solution, transdermal patch

Anorexiant

Phentermine is indicated as a short-term (a few weeks) adjunct therapy for weight reduction based on increased exercise, behavior modification, and calorie reduction.

phentermine (Adipex P) CIV - tablet, orally-disintegrating tablet, capsule

Stimulant

Modafinil may increase dopamine in the brain by decreasing dopamine reuptake. Modafinil is used for treating narcolepsy, shift work sleep disorder, treating Obstructive Sleep Apnea/Hypopnea Syndrome (OSAHS), and off label it is used fatigue in MS patients and for depression.

modafinil (Provigil) CIV - tablet

Antimanic Drug

Lithium is one of the oldest medications on the market for treating mania and is still quite popular. Lithium is also sometimes used to treat Huntington's disease, neutropenia (due to chemotherapy, or AIDS), cluster headache, PMS, bulimia, alcoholism, syndrome of inappropriate antidiuretic hormone secretion (SIADH), tardive dyskinesia, hyperthyroidism, and psychosis (postpartum or steroid-induced).

Lithium works by altering cation transport in nerve and muscle cells, and influences serotonin and/or norepinephrine reuptake.

Many of the antiepileptic drugs discussed later in this chapter are also often used as mood-stabilizing drugs.

lithium, LiCO3 (Eskalith, Lithobid) - tablet, extended-release tablet, capsule, syrup

NMDA Antagonist

N-methyl-D-aspartate (NMDA) antagonists prevent excessive stimulation of the NMDA-receptor, which is ordinarily stimulated by glutamate. At normal levels, glutamate aids in memory and learning, but if levels are too high, glutamate appears to overstimulate nerve cells, killing them through excitotoxicity.

Memantine has been associated with a moderate decrease in clinical deterioration with only a small positive effect on cognition, mood, behavior, and the ability to perform daily activities in moderate to severe Alzheimer's disease. There does not appear to be any benefit in mild disease.

memantine (Namenda) - tablet, extended-release capsule, oral solution

Other Psychiatry Agents

Atomoxetine is used to treat ADHD. It functions as a selective inhibitor of presynaptic norepinephrine transport. Unlike amphetamines used to treat ADHD, atomoxetine is considered to have little or no abuse potential.

atomoxetine (Strattera) - capsule

Antiepileptic drugs

Antiepileptic drugs (AEDs) will also sometimes be referred to as anticonvulsants. All of the drugs in this category can be used for treating various types of seizures and many of these medications have additional uses such as treating trigeminal neuralgia (carbamazepine), bipolar disorder (carbamazepine, lamotrigine, valproic acid), postherpetic neuralgia (gabapentin, pregabalin), muscle cramps (gabapentin), anxiety (gabapentin), diabetic neuropathy (gabapentin, pregabalin), fibromyalgia (pregabalin), neuropathic pain with spinal cord injury (pregabalin), migraine prophylaxis (topiramate, valproic acid), cluster-headache prophylaxis (topiramate), and alcoholism (topiramate).

carbamazepine (Tegretol, Equetro) - tablet, extended-release tablet, extended-release capsule, oral suspension
gabapentin (Neurontin) - capsule, tablet, oral solution
lamotrigine (Lamictal) - tablet, chewable tablet, orally-disintegrating tablet, extended-release tablet
levetiracetam (Keppra) - tablet, extended-release tablet, oral solution, injectable solution
oxcarbazepine (Trileptal) - tablet, extended-release tablet, oral suspension
pregabalin (Lyrica) CV - capsule, oral solution
topiramate (Topamax) - tablet, capsule
valproic acid (Depakote, Depakene, Depacon) - tablet, delayed-release tablet, extended-release tablet, capsule, delayed-release capsule, sprinkle capsule, syrup, injectable solution

Antiparkinson drugs

Parkinson disease is a common neurologic disorder affecting approximately 1% of the population over the age of 60 (a much smaller percentage of the population will sometimes have this disease at an earlier age) caused by the loss of dopamine receptors. This disease presents a number of motor and nonmotor symptoms related to the loss of dopamine receptors.

Typically, the first motor symptom is a resting tremor in an upper extremity. Over time, additional motor symptoms occur including bradykinesia, rigidity, and gait difficulty. The first affected arm may not swing fully when walking, and the foot on the same side may scrape the floor. As the disease progresses posture becomes increasingly flexed and strides become shorter causing a shuffling motion from the patient.

Nonmotor symptoms usually begin with the loss of smell, and is followed by rapid eye movements and behavior disorders.

The most common treatment is the use of carbidopa & levodopa to provide dopamine replacement therapy. Dopamine agonists, such as ropinirole, are also useful in decreasing the symptoms.

carbidopa & levodopa (Sinemet, Sinemet CR, Parcopa) - tablet, orally-disintegrating tablet, extended-release tablet
ropinirole (Requip, Requip XL) - tablet, extended-release tablet

Analgesics

Opioid Analgesics

Opioid analgesics are often used to treat acute pain (such as post-operative pain), and for palliative care to alleviate the severe, chronic, disabling pain of terminal conditions such as cancer, and sometimes for degenerative conditions such as rheumatoid arthritis. There has been an increased use of opioids in the management of non-malignant chronic pain. Opioids also have antitussive and antidiarrheal effects, therefore low doses and or weaker forms of these medications will sometimes be used for those purposes as well. These medications do have a potential for abuse due to their addictive nature. While addictive themselves, two of these medications (buprenorphine & naloxine and methadone) can be used to treat opioid addiction. Most of these medications are considered controlled substances and their federal schedules are listed beside them.

buprenorphine & naloxone (Suboxone) CIII - sublingual tablet, sublingual film
codeine CII - tablet, oral solution
codeine & acetaminophen (Tylenol with Codeine, Tylenol #3, Tylenol #4) CIII as a tablet and C5 as an oral solution - tablet, oral solution
fentanyl (Duragesic, Sublimaze, Actiq) CII - transdermal patch, injectable solution, sublingual tablet, buccal tablet, buccal film, sublingual solution, lollipop
hydrocodone & acetaminophen (Vicodin, Lorcet) CIII - capsule, tablet, oral solution, oral elixir
hydromorphone (Dilaudid) CII - tablet, extended-release tablet, injectable solution, oral solution, suppository, powder for injection
meperidine (Demerol) CII - tablet, injectable solution, syrup
methadone (Methadose, Dolophine) CII - tablet, dispersible tablet, oral solution, injectable solution
morphine (MS Contin, Duramorph, Kadian) CII - tablet, extended-release capsule, controlled-release tablet, oral solution, injectable solution, suppository
oxycodone (OxyContin, Roxicodone) CII - tablet, capsule, extended-release tablet, oral solution
oxycodone & acetaminophen (Percocet, Tylox, Roxicet) CII - tablet, capsule, oral solution
tramadol (Ultram) not federally scheduled - tablet, orally-disintegrating tablet, extended-release tablet, extended-release capsule
tramadol & acetaminophen (Ultracet) not federally scheduled - tablet

Non Steroidal Anti Inflammatory Drugs

Nonsteroidal anti-inflammatory drugs, usually abbreviated to NSAIDs are a class of drugs that provide analgesic and antipyretic effects, and, in higher doses, anti-inflammatory effects. NSAIDs are usually indicated for the treatment of acute or chronic conditions where pain and inflammation are present such as rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, dysmenorrhoea, headache and migraine, postoperative, inflammation, muscle stiffness, and fever.

celecoxib (Celebrex) - capsule
diclofenac (Voltaren, Cataflam) - tablet, extended-release tablet, capsule, powder packet for oral solution
ibuprofen (Advil, Motrin) - tablet, chewable tablet, oral suspension, injection solution
ketorolac (Toradol) - tablet, injectable solution
naproxen (Aleve, Naprosyn, Anaprox, Naprelan) - tablet, oral suspension
meloxicam (Mobic) - tablet, oral suspension
nabumetone (Relafen) - tablet
piroxicam (Feldene) - capsule

Miscellaneous Nonopioid Analgesics

Some medications do not easily fit into other categories such as acetaminophen, aspirin and some of the combination analgesics that contain weak barbiturates.

Acetaminophen, sometimes listed as APAP, is a potent analgesic and antipyretic activity with weak anti-inflammatory activity. Acetaminophen-containing products pose a potential to harm liver function and therefor patients are not to exceed a cumulative dose of 4 g/day of acetaminophen. In January 2011, the FDA mandated that all manufacturers limit acetaminophen in prescription products to 325 mg/dosage unit; manufacturers have until January 14, 2014, to comply.

Aspirin, sometimes listed as ASA, inhibits the synthesis of prostaglandin by cyclooxygenase; inhibits platelet aggregation; has antipyretic and analgesic activity. While aspirin could technically be classified as a NSAID, it is more often classified as a salicylate.

One thing that surprises many about the combination of butalbital, acetaminophen, and caffeine is that it is not federally scheduled even though butalbital, aspirin, and caffeine is considered a controlled substance.

acetaminophen (Tylenol) - tablet, extended-release tablet, chewable tablet, disintegrating tablet, elixir, suspension, suppository
aspirin (Bayer, Ascriptin, Bufferin, Ecotrin, St. Joseph Adult Chewable Aspirin) - tablet, delayed-release tablet, effervescent tablet, chewable tablet, suppository
butalbital, acetaminophen, & caffeine (Fioricet) - tablet, capsule, oral solution
butalbital, aspirin, & caffeine (Fiorinal) CIII - tablet, capsule

Serotonin 5-HT Receptor Agonist

Serotonin 5-HT receptor agonists cause vasoconstriction in cranial arteries to relieve migraines and cluster headaches.

rizatriptan (Maxalt) - tablet, disintegrating tablet
sumatriptan (Imitrex) - tablet, nasal spray, injectable solution
zolmitriptan (Zomig) - tablet, disintegrating tablet, nasal spray