Transcript Drugs II - Chemistry

The Most Prescribed Medications
by Class
http://pharma.about.com/od/Sales_and_Marketing/a/TheMost-Prescribed-Medications-By-Drug-Class.htm
Lipid Regulators
 Lipid regulators, mainly statin drugs, are used to
prevent dyslipidemia (high blood cholesterol) and
other cardiovascular problems and have been
prescribed for the prevention and treatment of many
other illnesses including osteoporosis and postmenopause complications. More than 255.4 million
prescriptions for statins and other lipid lowering
drugs were filled in 2010.
Lipid Regulators
 Pfizer's Lipitor (atorvastatin calcium) was the highest
selling branded statin, followed by Crestor
(rosuvastatin calcium) by AstraZeneca, Other branded
statins included Mevacor (lovastatin), Pravachol
(pravastatin sodium), Zocor (simvastatin), Lescol
(fluvastatin sodium), Vytorin (Ezetimibe/Simvastatin),
and Pitavastatin.
 Awareness campaigns directed at physicians and
directly to consumers have contributed to the growth
in this class of drugs.
Lipid Regulators
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Inhibiting cholesterol synthesis
Increasing LDL uptake
Decreasing of specific protein prenylation
Improve endothelial function
Modulate inflammatory responses
Maintain plaque stability
Prevent thrombus formation
Antidepressants
 Antidepressants are one of the fastest growing classes of
prescribed drugs. In 2010, more than 253.6 million
prescriptions were filled for antidepressants, according to
the IMS report.
 One of the main factors driving the increase in scripts for
antidepressants is that a growing number of primary care
providers and others practicing outside the field of
psychiatry are writing the prescriptions for patients who
have not received a clinical psychiatric diagnosis, according
to a study published in Health Affairs journal in August 2011
Antidepressants
 Selective serotonin reuptake inhibitors (SSRIs)
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sertraline (Zoloft)
fluoxetine (Prozac, Sarafem)
citalopram (Celexa)
escitalopram (Lexapro)
paroxetine (Paxil, Pexeva, Brisdelle)
fluvoxamine (Luvox)
trazodone (Oleptro)
Antidepressants
 Serotonin and norepinephrine reuptake inhibitors (SNRIs)
 SNRIs help improve serotonin and norepinephrine levels in
the brain. This may reduce depression symptoms. These
drugs include:
 duloxetine (Cymbalta)
 levomilnacipran (Fetzima)
 venlafaxine (Effexor XR)
In addition to treating depression, duloxetine (Cymbalta) may
also relieve pain. This is important because chronic pain can lead
to depression or make it worse.
Antidepressants
 Tricyclic antidepressants (TCAs)
 TCAs are often prescribed when SSRIs or other
antidepressants don’t work. It isn’t fully understood
how these drugs work to treat depression.
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amitriptyline
amoxapine
clomipramine (Anafranil)
desipramine (Norpramin)
Antidepressants
 Other medications for depression - Tetracyclic
antidepressant
 Maprotiline is used to treat depression and anxiety. It
also works by balancing neurotransmitters to ease
symptoms of depression.
Antidepressants
 Dopamine reuptake blocker
 Bupropion (Wellbutrin, Forfivo, Aplenzin) is a mild
dopamine and norepinephrine reuptake blocker. It’s
used for depression and seasonal affective disorder
(SAD). It’s also used in smoking cessation.
Antidepressants
 5-HT2 receptor antagonists
 Two 5-HT2 receptor
antagonists, nefazodone and trazodone, are used to
treat depression. These are older drugs. They alter
chemicals in your brain to help depression.
 5-HT3 receptor antagonists
 One 5-HT3 receptor antagonist, vortioxetine
(Brintellix), treats depression by affecting the activity
of brain chemicals.
Antidepressants
 Monoamine oxidase inhibitors (MAOIs)
 MAOIs are older drugs that treat depression. They
work by stopping the breakdown of norepinephrine,
dopamine, and serotonin. They’re more difficult for
people to take than most other antidepressants. This
is because they interact with prescription drugs,
nonprescription drugs, and some foods. They also
can’t be combined with stimulants or other
antidepressants.
Antidepressants
 isocarboxazid (Marplan)
 phenelzine (Nardil)
 selegiline (Emsam), which comes as a transdermal
patch
 tranylcypromine (Parnate)
Narcotic Analgesics
 Narcotic analgesics are prescribed for the relief of severe pain. In
2010, more than 244,300,000 prescriptions were filled for these
types of pain killers.
 Examples of narcotic analgesics are:
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codeine,
hydrocodone (Zohydro ER),
oxycodone (OxyContin, Roxicodone),
methadone,
hydromorphone (Dilaudid, Exalgo),
morphine (Avinza, Kadian, MSIR, MS Contin), and
fentanyl (Actiq, Duragesic).
Narcotic Analgesics
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Big problems!!! Significant abuse potential.
Addiction and overdose
Narcan: Opiate antagonist
http://www.dailymail.co.uk/news/article3444210/New-Jersey-mother-dying-heroin-overdosesaved-Narcan-antidote.html#v-7343188617160245960
Narcotic Analgesics
 Mode of action - All opioid analgesics mimic endogenous
(meaning produced by the human body) endorphins by
stimulating opioid receptors in the central and peripheral
nervous systems which results in relief of pain. Opioids are
particularly useful in pain management as they:
 Can be given by a variety of routes including oral,
transmucosal, rectal, intravenous, subcutaneous,
intramuscular, transdermal, epidural and intrathecal;
 Are easily titrated to the correct dose;
 Are highly effective;
 Have a favorable risk benefit ratio.
Narcotic Analgesics
Beta Blockers
 Beta-adrenergic blocking agents or beta
blockers (plain and in combination with other
drugs, are prescribed for the treatment of
heart disease, particularly high blood
pressure, as well as glaucoma,
hyperthyroidism and migraines. More than
191.5 million prescriptions for beta blockers
were filled in 2010
Beta Blockers
 Commonly prescribed beta blockers include Brevibloc
(esmolol), Coreg (carvedilol), Inderal (propranolol),
Lopressor, Toprol-XL (metoprolol), Normodyne,
Trandate (labetalol), Sectral (acebutolol), Tenormin
(atenolol) and Zebeta (bisoprolol).
Beta Blockers
Ace Inhibitors
 Angiotensin-converting enzyme (ACE) inhibitors are used
in the treatment of high blood pressure, scleroderma,
migraines and other conditions. In 2010, pharmacies
dispensed more than 168.7 million prescriptions for ACE
inhibitors.
 Angiotensin-converting enzyme (ACE) inhibitors help
relax blood vessels. ACE inhibitors prevent an enzyme in
your body from producing angiotensin II, a substance in
your body that narrows your blood vessels and releases
hormones that can raise your blood pressure.
Antidiabetes
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Let’s talk about diabetes – huge healthcare costs
2 types
Common drugs?
Insulin – what does it do?
Respiratory agents
 Respiratory agents are drugs or a combination of
drugs used to prevent, relieve or treat respiratory
diseases. They can be taken as pills or liquid, for the
drugs to work systemically. Or they can be available
as inhalers or other forms or inhalation devices,
where the medicine is delivered directly into the lungs
Respiratory agents
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antiasthmatic combinations - asthma
Antihistamines – allergies/sensitivities
Antitussives – Coughing
Bronchodilators
Decongestants
Expectorants - gets the phlegm out
leukotriene modifiers - manage allergic rhinitis or allergies, as well as prevent asthma
lung surfactants
miscellaneous respiratory agents
respiratory inhalant products
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inhaled anti-infectives
inhaled corticosteroids
mast cell stabilizers
mucolytics
Antacids, Antireflux Agents &
Antiulcerants
 Antacids are salts of magnesium, aluminium and
calcium used to neutralize the gastric acid and raise
the gastric pH to treat dyspepsia and also provide
symptomatic relief for peptic ulcer disease and
gastro-esophageal reflux disease (GERD). Anti-reflux
and Anti-ulcerant drugs are a class of drugs called
proton pump inhibitors and histamine receptor
blockers that stop acid secretion at the source of
production and are used to treat ulcers in the
stomach and the upper part of the small intestine and
GERD.
High Blood Pressure and Diuretics
(Water Pills)
 For high blood pressure, diuretics, commonly known
as "water pills," help your body get rid of unneeded
water and salt through the urine. Getting rid of excess
salt and fluid helps lower blood pressure and can
make it easier for your heart to pump. Diuretics may
be used to treat a number of heart-related conditions,
including high blood pressure, heart failure, kidney
and liver problems, and glaucoma.
High Blood Pressure and Diuretics
 Thiazide diuretics, such as Esidrix or Zaroxolyn, can be used to lower
blood pressure, or to treat edema in heart failure.
 Loop diuretics (Lasix, Bumex) are often used when people have
congestive heart failure symptoms and are especially useful in
emergencies. However, they do not significantly lower blood
pressure.
 Potassium-sparing diuretics (like Aldactone, Dyrenium) help your
body retain potassium and are used more often in congestive heart
failure patients. They are often prescribed in conjunction with the
other two types of diuretics, but also do not significantly lower
blood pressure.
Anti-Epileptics
 Anti-epileptic drugs (AEDs) are the main form of
treatment for people with epilepsy.
 https://www.epilepsysociety.org.uk/list-anti-epilepticdrugs#.V6QUeNIrI-k
 Life altering!!!!
Tranquilizers
 Medically, barbiturates are prescribed for acute
anxiety, tension and sleep disorders. Benzodiazepines
are prescribed for anxiety, acute stress reactions, and
panic attacks.
 Some potential for abuse!
Antirheumatics
 Antirheumatics include drugs, which are used to treat
the symptoms of rheumatoid arthritis and those that
can modify the course of the disease. The drugs that
help treat the symptoms such as pain and
inflammation are aspirin, non-steroidal antiinflammatory drugs (NSAIDs) and steroids. Drugs that
can slow the progression of rheumatoid arthritis and
help with pain, inflammation and stiffness are called
disease modifying rheumatoid arthritis drugs
(DMARDs).
Antirheumatics
 These drugs frequently modify the bodies’ own
immune response: the list of possible side effects are
shocking
 https://www.youtube.com/watch?v=IFrl-Kbe6wI
Antibiotics
 Taken for bacterial infection
 Do you take an antibiotic for the flu?
 Do you take an antibiotic for a cold?
 Do you take an antibiotic for pneumonia?
Antibiotics
Bringing a new drug to market
 $2.6 billion
 A new report published by the Tufts Center for the
Study of Drug Development (CSDD) pegs the cost of
developing a prescription drug that gains market
approval at$2.6 billion, a 145% increase, correcting for
inflation, over the estimate the center made in 2003.
 http://www.scientificamerican.com/article/cost-todevelop-new-pharmaceutical-drug-now-exceeds-2-5b/
Bringing a new drug to market
Process for bringing a drug to market
 www.fda.gov/ohrms/.../ac/.../3996S1_08_Rosario.PPT
Accidental Drug discoveries
 http://io9.gizmodo.com/5871300/10-happy-accidentsfrom-the-annals-of-drug-discovery