Drugs of Shame Series

How about starting the series with a Doctor of Shame who in the ER gave to a migraineur 3 Drugs of Shame?

Imagine that you are in horrific pain! You are also partially blinded by the pain and parts of your body are paralyzed because you have hemiplegic migraines. You head to the ER and the resident neurologist gives you the following three medications:

Tramadol, Ergotamine tartrate, and Propranolol

Before I give you the details of the drugs in brief, I show you what I could find simply by placing the 3 drug names into an online dug interaction checker:

Interactions for the following two medications I put in there:

“Tramadol and Ergotamine tartrate

Interactions  All (1)  Significant (1)

Ergotamine tartrate + Tramadol

Ergotamine tartrate and Tramadol both increase serotonin levels in the blood. Too much serotonin is a potentially life-threatening condition. Severe signs and symptoms include high blood pressure and increased heart rate that lead to shock.”

So your doctor is giving you two medications that both achieve the same chemical alterations in the brain: overdose by duplication. One of the side effects of such overdose is an increased blood pressure by blood vessel constricting so the third medicine, Propranolol, is doing what? Reduce blood pressure? Nah… It increases it further! It is a strong vasoconstrictor that is not even supposed to be given to a low blood pressure patient (the migraineur in questions has typical blood pressure of 90/60, way below normal!). So as you see, a clueless doctor can sure make a mess of already shameful drugs!

These 3 drugs will be revisited later in greater detail but for now in brief, I just explain the main functions and how they work so you can see the cluelessness. Later each drug will have its own decorated page under Drugs of Shame. The purpose of this introduction to Drugs of Shame is to show you how many doctors have absolutely no clue what the drugs they prescribe do and by what mechanism.

The three medicines in brief:

Tramadol: is an opioid that binds to the μ-opioid receptor and also acts as a serotonin and norepinephrine reuptake inhibitor so it is an SNRI. Inhibiting reuptake in the brain is synonymous with plugging the overflow in your sink or tub. When the brain had enough serotonin and norepinephrine already, it does not know about it because its overflow hole (reuptake) is plugged (inhibited). Hence the brain continues to make these neurotransmitters thinking it needs to make more. This in turn overflows the brain with serotonin and norepinephrine endlessly, 24/7. Tramadol alone is already troubling and can cause serotonin syndrome on its own.

Ergotamine (Ergot for short): is structurally similarity to several neurotransmitters like serotonin at the5-HT1A receptors, dopamine at the D2 receptor and epinephrine, and can thus bind to several receptors acting as an agonist. Agonists “excite” the receptors to take up more. So one medication is already flooding the brain (Tramadol) with these neurotransmitters forcing the brain receptors to sponge up as much as they can and now they are instructed to sponge up more and more!  At the same time Ergot acts as a vasoconstrictor as well. It works by constricting the intracranial extracerebral blood vessels through the 5-HT1B receptor and by inhibiting trigeminal neurotransmission by 5-HT1D receptors. This not only causes a double dose (overdose) but also causes the BP to increase.

Propranolol (Inderal) is a beta blocker that increases blood pressure by vasoconstriction achieved by vasospasm. Vasospasm refers to a condition in which a blood vessel’s spasm leads to vasoconstriction. This can lead to tissue ischemia and tissue death (necrosis). Cerebral vasospasm may arise in the context of subarachnoid hemorrhage. Propranolol is not recommended for the treatment of hypertension because of its relatively high rate of cardiovascular death, myocardial infarction, or stroke. Propranolol has inhibitory effects on the norepinephrine transporter and/or stimulates norepinephrine release (? which one??? So we know what we prescribe?). Propranolol increases synaptic norepinephrine at the α-adrenergic receptors so this is yet one more medicine that double doses—or rather in this case triple doses since all three drugs contribute to norepinephrine release. In addition propranolol may function as a partial agonist at some serotonin receptors. Propranolol also blocks the voltage-gated sodium channels.

In quick summary:

• Tramadol forces neurons to make two neurotransmitters: serotonin and norepinephrine and increases blood pressure by its vasoconstriction. It is also an opioid.
• Ergotamine increases serotonin, dopamine, epinephrine and has a vasoconstriction action.
• Propranolol is a vasoconstrictor that either inhibits or stimulates norepinephrine (we don’t know which?) and most importantly it blocks voltage-gated-sodium-channels. Voltage gated sodium channels are necessary to manufacture neurotransmitters!

So 2 drugs are given to load the brain with neurotransmitters and the 3^rd drug prevents that!

Note also that all three constrict blood vessels and increase blood pressure that can cause stroke and other harm. All three take part in modifying brain neurotransmitters in some way that have serious consequences to our body, not one of which has anything to do with reducing migraines! Not one of these drugs is expressly for migraines albeit off label they have been used so.

Migraine is a special brain with enhanced sensory neuron connections (migraineurs smell better, hear better, see better in dark so light bothers them), etc. So their brains need different energy for their heightened activity! The energy they need is extra voltage and not neurotransmitter release enforcement guards with blood pressure increasing!

Please read my book to understand what a migraine brain is! Do yourself a favor: when you are hit with a migraine or know someone who has migraines, please buy them the book Fighting the Migraine Epidemic or have them send a message to me via the comment option below! I am glad to help! Save your life and run from doctors!

Your comments are welcome as always!

Angela