We use the highest quality and FDA approved ingredients when formulating our compounded medications. Our skillfully trained pharmacists will work directly with your healthcare provider to ensure the active ingredients selected for your custom compounded medication are most suitable for your specific needs. Due to the complex nature of pain, the use of multiple agents with complimentary modes of action is often key to the success of transdermal therapy. The ultimate goal is to pick the combination of ingredients that result in the best therapeutic outcome, by working closely with the patient, prescriber, and compounding pharmacist.
1.) Acyclovir – For patients with shingles or postherpetic pain, the addition of the antiviral drug acyclovir (in concentrations of 5%) can be very effective. Combine with gabapentin and ketamine for postherpetic pain.
2.) Amitriptyline – Amitriptyline is a tricyclic antidepressant agent. It is has been used extensively as an analgesic agent for management of neuropathic pain. Unfortunately, the higher oral doses needed to achieve an analgesic effect cause somnolence and dry mouth, thus limiting patient tolerance and compliance. Side effects are eliminated following topical administration. Amitriptyline is used topically in concentrations of 2-5%.
3.)Baclofen – Baclofen is a GABA β receptor agonist. GABA receptor agonists primarily cause muscle relaxation. Baclofen is commercially available as an oral tablet and an intrathecal injection. Baclofen helps reduce painful muscle spasms and clonus in patients with multiple sclerosis and other musculoskeletal conditions. Baclofen is used topically in concentrations of 1-2%. Baclofen is effective but expensive.
4.)Clonidine – Although the precise mechanism of action is unknown, it is believed that clonidine may decrease the site-specific local release of norepinephrine, an agent that stimulates sensitized nerve fibers to cause painful sensations. Clonidine is used orally to treat hypertension, but is also given by epidural or intrathecal injection to help control pain. It is not effective for pain when taken orally. Clonidine’s topical effects were discovered when some patients experienced pain relief following the application of the clonidine-TTS patch. Unfortunately, the effects were very localized, thus limiting the usefulness of the patch. However, the ability to apply clonidine directly to the pain site or dermatome is a significant advantage of our cream formulations. Clonidine is used topically in concentrations of 0.1 – 0.2%.
5.) Cyclobenzaprine – Cyclobenzaprine (trade name Flexeril® ) is structurally similar to the tricyclic antidepressants (such as amitriptyline). It is prescribed orally to relieve muscle pain and stiffness caused by injuries such as sprains or strains. When incorporated into creams it is reported to be very effective in relieving muscle tightness in patients with Fibromyalgia Syndrome (FMS) and multiple sclerosis. Cyclobenzaprine is used in a concentration of 1- 2%.
6.) Gabapentin – Gabapentin (trade name Neurontin® ) is an antiepileptic medication used to control seizures. There have long been recognized similarities with neuronal misfiring in epilepsy and neuropathic pain. Phenytoin, a commonly prescribed anticonvulsant medication, was shown to have analgesic effect in neuropathic pain in 1942. In neuropathic pain, injured nerve fibers may discharge spontaneously – usually at regular intervals – causing significant pain. Gabapentin is a glutamate antagonist. Glutamate is the chemical that stimulates the NMDA pain receptors (see ketamine section below). Blocking glutamate blocks pain transmission. When administered orally (dosage range of 2400-3600mg/day), Gabapentin has shown results in managing pain caused by diabetic neuropathy and postherpetic neuralgia. Topically, the concentrations used are around 5-6%. Gabapentin is very effective and is well tolerated. It should be considered as a mainstay ingredient for all neuropathic pain creams.
7.)Guaifenesin – Oral guaifenesin is used as an expectorant to decrease viscosity of respiratory secretions. Topically, guaifenesin is an effective skeletal muscle relaxant. Concentrations used are 5-10%.
8.)Ketamine – Ketamine is an N-methyl-D-aspartate (NMDA) receptor antagonist and is topically used in concentrations of 6%. When the pain receptors in the dermatomes start sending signals there is a release of glutamate, which in turn acts on the NMDA receptors in the spinal cord. Activation of NMDA receptors causes the spinal cord neurons to become even more sensitive and responsive to painful stimuli. Ketamine works on receptors in the both the periphery and in the spinal cord. There is also new evidence that blocking NMDA receptors with drugs such as ketamine decreases the development of tolerance to opioids such as morphine, hydrocodone (Vicodin® ), and fentanyl (Duragesic® ). Ketamine is another one of the core drugs used in our topical pain cream formulations.
9.)Ketoprofen – Concentrations of 5-10% are commonly prescribed. Ketoprofen is a NSAID and provides excellent relief for acute inflammation and swelling resulting from soft-tissue and skeletal muscle injuries. It should be included as an ingredient whenever inflammation is suspected. Ketoprofen cream is particularly effective for treating arthritis inflammation in the back, hands, knees, or other joints. Ketoprofen cream is also effective for patients with gouty arthritis.
10.)Orphenadrine – Orphenadrine is a muscle relaxant with NMDA antagonist activity. Topical concentrations used are 5-10%. It is reported to block pain transmission and cause muscle relaxant effects.
11.)Pentoxifylline – Pentoxifylline is a Tumor Necrosis Factor antagonist (TNF-1α). Tumor necrosis factor is a substance produced primarily by monocytes and macrophages in response to inflammatory processes such as arthritis. Topical pentoxifylline reduces inflammation by inhibiting TNF at the cellular level. It is a useful ingredient whenever inflammation is present. Sciatica and neuropathic pain also respond well to pentoxifylline administration. Concentrations used are 5-10%.
12.)Piroxicam – Piroxicam is a potent NSAID. Like other NSAIDs, it provides relief for acute inflammation and swelling resulting for soft-tissue and skeletal muscle injuries. Topical concentrations used on 0.5 - 1%. We frequently combine piroxicam and ketoprofen for patient’s whose pain is primarily inflammatory in origin.
13.)Tetracaine & Lidocaine – Both of these drugs are local anesthetics that have neuron membrane stabilizing effects. Lidocaine is currently available as a 5% transdermal patch (Lidoderm® ) approved for management of postherpetic neuralgia. Tetracaine concentrations used in the pain formulations are 1-2%. Lidocaine concentrations used are 2-5%.
*Due to the medications used in formulating our Transdermal Pain Cream, this medication is available by prescription only.