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[[Image:DrugPk.png|600px|thumb|right|Diagram of Drug Concentration with key PK characteristics highlighted]]
[[Image: Nexium.jpg|160px|right|thumb|AstraZeneca’s Nexium]]
The Pharmaceutical industry is one of the world’s largest industries, grossing well over $300 billion in the United States alone. Understanding how the drugs the pharma industry develops work and different characteristics of these compounds is important to nearly everyone as 50% of the US population takes at least one prescription medication regularly and nearly everyone takes a pharmaceutical pill at some point in their life.<ref>http://www.npr.org/blogs/health/2010/09/03/129626052/a-portrait-of-health-prescription-drugs-in-america</ref>  
The Pharmaceutical industry is one of the world’s largest industries, grossing well over $300 billion in the United States alone. Understanding how the drugs the pharma industry develops work and different characteristics of these compounds is important to nearly everyone as 50% of the US population takes at least one prescription medication regularly and nearly everyone takes a pharmaceutical pill at some point in their life.<ref>http://www.npr.org/blogs/health/2010/09/03/129626052/a-portrait-of-health-prescription-drugs-in-america</ref> See also [[WHO Model Lists of Essential Medicines]]. The following is a growing list of pharmaceutical compounds organized by disorder.  
 
This page will serve as a simple explanation of how specific pharmaceutical compounds work and what their “pharmacokinetic” characteristics are.<ref>http://www.pharmpress.com/shop/samples/clinical_pharmacokinetics_samplechapter.pdf</ref> <br />
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<br />
<br/>
See [[Pharmaceutical Drug Targets]] for a list of drug targets organized by disease.  
See [[Pharmaceutical Drug Targets]] for a list of drug targets organized by disease.  
 
<br />
==Pharmacokinetics Translated==
<br/>
Pharmacokinetics (PK) measures the variations of drug levels in the body with relation to how much compound you take and time since taking the drug.
The majority of all modern medicinal drugs target members of the superfamily of proteins called the [[G protein-coupled receptor|G protein-coupled receptors]] or GPCRs<ref name="howmany">PMID: 17139284</ref><ref name="pharmtrends">PMID: 21075459</ref>.
 
===Bioavailability (F)===
This is the amount of a drug that actually makes it into your bloodstream as compared to the amount you put in your mouth, inhale, or inject. Since the body has dozens of defense mechanisms to keep foreign compounds out of your blood, simply getting the active compound into your bloodstream is pretty difficult. Drug compounds must pass through the hostile stomach, must avoid setting off an immune response, must avoid being metabolized by the liver and ultimately be absorbed by the small intestine in order to make it into the blood.
 
====Protein Binding====
Once a drug compound has successfully entered the blood stream, an important consideration is how much of the drug is freely available to enter cells versus how much is bound by plasma proteins. Proteins bind drug compounds at varying rates, decreasing the rate at which drug compounds are absorbed by cells. Without such proteins, many compounds, like adrenaline, would be absorbed too fast and would not reach all of the targets in the body. Many drugs are so completely bound by protein that their availability toward absorption by cells is nearly zero.
 
====Barriers====
Certain parts of the body have barriers to entry. Cell membranes for example have a highly hydrophobic interior which excludes polar molecules to enter. Thus most drugs must pass into cells through [[Membrane Channels & Pumps|membrane channels and membrane transport proteins]]. Another important barrier is the so-called “blood brain barrier”, which protects your brain and spinal cord from toxins. This is a good thing as the brain is a sensitive place, but it can be detrimental to pharmaceutical scientists attempting to develop a compound to function in the brain.
 
===Dose (D)===
Quite simply it is the mass of active compound you take, typically measured in mg.
 
===Concentration (C<sub>0</sub>) or (C<sub>ss</sub>)===
It's either the initial or steady state concentration of the drug in the blood plasma.
 
====C<sub>max</sub>====
This is the peak concentration of a drug after administration. It is related to the short-term side effects of the drug which typically include nausea, or lethargy.
 
====C<sub>min</sub>====
This is the lowest concentration a drug reaches before a second administration of the drug occurs. Most manufacturers try to maintain a C<sub>min</sub> about 3 times the IC<sub>50</sub> to allow for a "buffer" room above the critical effectiveness cutoff.
 
===Half Life (T<sub>1/2</sub>)===
Typically measured in hours, it is the time required for the concentration of the drug in your blood to be reduced by ½. Once a drug enters the blood, the body will immediately start to remove it. T<sub>1/2</sub> gives an indication of how long the drug will be active for.
 
===T<sub>max</sub>===
How long after taking the drug does the drug hit its C<sub>max</sub>, typically measured in hours. It is a measure of how long you have to wait before the drug hits maximum effectiveness along with when you can expect short term side effects to reach their peak.
 
===Clearance (Cl)===
This is a measure of the volume of plasma cleared of the drug per unit of time. In other words, how much of your blood is rid of the drug per unit of time.
 
===Area Under the Curve (AUC)===
This is a measurement of the total exposure someone has to the drug. It is represented by the area under the PK curve. It is the integral of the concentration over time. It is related to the long-term side effects of a drug, i.e. greater exposure to any foreign compound, the more likely long-term side effects are.
 
===Inhibitory Concentration (IC<sub>50</sub>)===
This is a measurement of the half maximal inhibitory concentration. In other words, it is a measure of how much drug must be taken before 50% of the particular biochemical function is inhibited. It is the typical measurement of drug potency in which lower values indicate increased potency.


==Treatments==
==Treatments==
The following is a list of FDA Approved treatments for various diseases, organized by disorder. Each entry highlights general information about the therapeutic, pharmacokinetic data comparisons within its drug class, and a structural analysis explaining how the drug compound functions ''in vivo''.
The following is a list of pharmaceutical treatments for various diseases, organized by disorder. Each entry highlights general information about the therapeutic, [[Pharmacokinetics|pharmacokinetic data]] comparisons within its drug class, and a structural analysis explaining how the drug compound functions ''in vivo''.
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==[[Diabetes]]==
==Depression==
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<td style="width:33%;border-width:1px; border-style:inset; text-align:center;background:#F1F2FC">
==Erectile Dysfunction
==[[Diabetes]]==
</td>
</td>
<td style="width:33%;border-width:1px; border-style:inset; text-align:center;background:#F1F2FC">
<td style="width:33%;border-width:1px; border-style:inset; text-align:center;background:#F1F2FC">
==[[Hypercholesterolemia]]==
==Erectile Dysfunction==
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{{:Treatments:Depression}}
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==[[Hypercholeseterolemia]]==
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==[[Hypertension]]==
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==[[HIV]]==
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{{:Treatments:Hypercholeseterolemia}}
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{{:Treatments:Hypertension}}
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{{:Treatments:HIV}}
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==[[Hypertension]]==
==[[Inflammation & Rheumatoid Arthritis|Inflammation & Arthritis]]==
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==[[HIV]]==
==[[Influenza]]==
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==[[Influenza]]==
==[[Opioids|Opioid drugs]]==
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{{:Treatments:Inflammation}}
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{{:Treatments:Influenza}}
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{{:Treatments:Opioid drugs}}
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==Viral diseases==
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<td style="width:33%;border-width:1px; border-style:inset; text-align:center; background:#F1F2FC">
==Asthma==
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<td style="width:33%;border-width:1px; border-style:inset; text-align:center; background:#F1F2FC">
==Various diseases==
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{{:Treatments:HIV}}
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====Coming Soon...====
Tamoxifen <br />
Cozaar <br />
Januvia <br />
Azithromycin <br />
Puromycin <br />
Tamiflu <br />
Relenza <br />
Teleprevir <br />
Rituxan <br/>
Arzerra <br/>
Gleevec <br />
Taxol <br />
Lipoderm <br />
Paxil <br/>
Viagra <br />
Cialis <br />
Celebrex <br />
Vioxx <br />
Herceptin <br />
 


==References==
===References===
<references/>
<references/>
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Latest revision as of 12:53, 9 January 2025

AstraZeneca’s Nexium

The Pharmaceutical industry is one of the world’s largest industries, grossing well over $300 billion in the United States alone. Understanding how the drugs the pharma industry develops work and different characteristics of these compounds is important to nearly everyone as 50% of the US population takes at least one prescription medication regularly and nearly everyone takes a pharmaceutical pill at some point in their life.[1] See also WHO Model Lists of Essential Medicines. The following is a growing list of pharmaceutical compounds organized by disorder.

See Pharmaceutical Drug Targets for a list of drug targets organized by disease.

The majority of all modern medicinal drugs target members of the superfamily of proteins called the G protein-coupled receptors or GPCRs[2][3].

Treatments

The following is a list of pharmaceutical treatments for various diseases, organized by disorder. Each entry highlights general information about the therapeutic, pharmacokinetic data comparisons within its drug class, and a structural analysis explaining how the drug compound functions in vivo.

Alzheimer's Disease

Bacterial Infection

Cancer
Acetylcholinesterase Inhibitors
Antagonists at glutamatergic NMDA receptors
Antibiotics
Anti-ulcer antibiotics
Beta-lactam antibiotics

See Beta-lactam antibiotics, Penams

Anti-CD20 Monoclonal Antibody
Anti-melanoma Monoclonal Antibody

See Treatment of multiple myeloma

Anti-prostate cancer
Anti-myeloma
Anti-acute lymphocytic leukemia
Anti-non-small cell lung cacinoma
B-Raf Kinase Inhibitor
  • Zelboraf - Generic: Vemurafenib (Formerly: PLX-4032)
Chemotherapy
Dihydrofolate Reductase Inhibitor
Epidermal Growth Factor Receptor Inhibitors
Estrogen Receptor Modulator
mTOR inhibitor
  • Rapamune - Generic: Sirolimus (Rapamycin)
  • Afinitor - Generic: Everolimus
  • Torisel - Generic: Temsirolimus
Multiple Receptor Tyrosine kinase (VEGFR, PDGFR, EGFR, KIT, Abl, RAF kinase) Inhibitors

See Treatment of chronic myelogenous leukemia, Treatment of hepatocellular carcinoma, Treatment of renal cell carcinoma, Treatment of gastrointestinal stromal tumor, VEGFR inhibitors and Tyrosine-kinase inhibitors.

Vascular Endothelial Growth Factor Inhibitor
Poly ADP ribose polymerase (PARP) inhibitors
Cyclin-dependent kinases inhibitors

See also Anti-cancer drugs, Anticancer drugs and RAF kinase inhibitors

Depression

Diabetes

Erectile Dysfunction

Serotonin Transporter Inhibitors

Tricyclic Antidepressants
Selective Serotonin Reuptake Inhibitors
Serotonin–norepinephrine reuptake inhibitor
Serotonin–dopamine reuptake inhibitor

See Atypical antipsychotics


Insulin
Dipeptidyl peptidase IV Inhibitor
Peroxisome Proliferator-Activated Receptor Agonist
Glucagon-like peptide-1 (GLP-1) agonist
Mechanism is not completely understood
Inhibitors of the sodium glucose co-transporter-2 (SGLT-2)
Phosphodiesterase Type 5 Inhibitor
  • Cialis - Generic: Tadalafil
  • Levitra - Generic: Vardenafil
  • Viagra - Generic: Sildenafil

Hypercholeseterolemia

Hypertension

HIV
HMG-CoA Reductase Inhibitors (Statins)
Niemann-Pick C1-like 1 (NPC1L1) protein blocker
Angiotensin-Converting Enzyme Inhibitors
β-Adrenergic Receptor Antagonists
Ionotropic Glutamate Receptors
Inhibitors of neprilysin
Renin inhibitors
Angiotensin II receptor antagonist
Chemokine Receptor Type 5 (CCR5) Inhibitors
  • Selzentry - Generic: Maraviroc
HIV-Protease Inhibitors
Non-Nucleoside Reverse Transcriptase Inhibitors
Nucleoside Analog Reverse Transcriptase Inhibitors
  • Baraclude - Generic: Entecavir
  • Emtriva - Generic: Emtricitabine
  • Epivir - Generic: Lamivudine
  • Hivid - Generic: Zalcitabine
  • Retrovir - Generic: Zidovudine
  • Videx - Generic: Didanosine
  • Viread - Generic: Tenofovir
  • Zerit - Generic: Stavudine
  • Ziagen - Generic: Abacavir
Retroviral Integrase Inhibitors
Cytochrome P450 inhibitors
Combinations


Inflammation & Arthritis

Influenza

Opioid drugs
Cyclooxygenase Inhibitors
Phospholipase A2 Inhibitors
  • Voltaren - Generic: Diclofenac also may inhibit phospholipase A2 as part of its mechanism of action.
M2 Proton Channel Inhibitors
Neuraminidase Inhibitors
Opioid receptors agonists
  • MScontin, Oramorph, Sevredol - Generic: Morphine (opioid receptor agonist)
  • Demerol - Generic: Meperidine (opioid receptor agonist)
  • Dolophine - Generic: Methadone (Levomethadone (the R enantiomer) is a opioid receptor agonist)
  • Actiq, Duragesic, Fentora - Generic: Fentanyl (opioid receptor agonist)
Opioid receptors antagonists
  • Narcan - Generic: Naloxone (competitive opioid receptor antagonist)
  • ReVia - Generic: Naltrexone (competitive opioid receptor antagonist)
  • Entereg - Generic: Alvimopan (opioid receptor antagonist)

Viral diseases

Asthma

Various diseases


References

  1. ↑ http://www.npr.org/blogs/health/2010/09/03/129626052/a-portrait-of-health-prescription-drugs-in-america
  2. ↑ Overington JP, Al-Lazikani B, Hopkins AL. How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. PMID:17139284 doi:10.1038/nrd2199
  3. ↑ Peeters MC, van Westen GJ, Li Q, IJzerman AP. Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation. Trends Pharmacol Sci. 2011 Jan;32(1):35-42. PMID:21075459 doi:10.1016/j.tips.2010.10.001


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David Canner, Wayne Decatur, Alexander Berchansky, Karsten Theis, Michal Harel
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